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A Stereoselective Synthesis of the ACE Inhibitor Trandolapril

S. Chiha, M. Spilles, J. r.-M. Neudörfl, H.-G. n. Schmalz, Synlett 2019, 30, A-D. 10.1055/s-0037-1612306


A conceptually novel and stereoselective synthesis of the en- antiopure octahydroindole building block and its conversion into the ACE inhibitor trandolapril was achieved. Key steps include the -allyla- tion of a protected L-pyroglutamic acid derivative, a highly diastereose- lective Hosomi–Sakurai reaction and a Ru-catalyzed ring-closing me- tathesis of a 4,5-diallylated proline. This way, the synthesis of trandolapril was efficiently achieved in 25% overall yield (12 steps).


Inhibition of CPAP-tubulin interaction prevents proliferation of centrosome-amplified cancer cells

A. Mariappan, K. Soni, K. Schorpp, F. Zhao, A. Minakar, X. Zheng, S. Mandad, I. Macheleidt, A. Ramani, T. Kubelka, M. Dawidowski, K. Golfmann, A. Wason, C. Yang, J. Simons, H.-G. Schmalz, A. A. Hyman, R. Aneja, R. Ullrich, H. Urlaub, M. Odenthal, R. Buettner, H. Li, M. Sattler, K. Hadian, J. Gopalakrishnan, EMBO J. 2019, 38, n/a. 10.15252/embj.201899876


Centrosome amplification is a hallmark of human cancers that can trigger cancer cell invasion. To survive, cancer cells cluster amplified extra centrosomes and achieve pseudobipolar division. Here, we set out to prevent clustering of extra centrosomes. Tubulin, by interacting with the centrosomal protein CPAP, negatively regulates CPAP‐dependent peri‐centriolar material recruitment, and concurrently microtubule nucleation. Screening for compounds that perturb CPAP–tubulin interaction led to the identification of CCB02, which selectively binds at the CPAP binding site of tubulin. Genetic and chemical perturbation of CPAP–tubulin interaction activates extra centrosomes to nucleate enhanced numbers of microtubules prior to mitosis. This causes cells to undergo centrosome de‐clustering, prolonged multipolar mitosis, and cell death. 3D‐organotypic invasion assays reveal that CCB02 has broad anti‐invasive activity in various cancer models, including tyrosine kinase inhibitor (TKI)‐resistant EGFR‐mutant non‐small‐cell lung cancers. Thus, we have identified a vulnerability of cancer cells to activation of extra centrosomes, which may serve as a global approach to target various tumors, including drug‐resistant cancers exhibiting high incidence of centrosome amplification.

An Atom-Economic and Stereospecific Access to Trisubstituted Olefins through Enyne Cross Metathesis Followed by 1,4-Hydrogenation

F. Ratsch, H.-G. Schmalz, Synlett 2018, 29, 785-792. 10.1055/s-0036-1591528


The combination of intermolecular enyne cross metathesis and subsequent 1,4-hydrogenation opens a stereocontrolled and atom-economic access to trisubstituted olefins. By investigating different combinations of functionalized alkyne and alkene substrates, we found that the outcome (yield, E/Z ratio) of the Grubbs II-catalyzed enyne cross-metathesis step depends on the substrate’s structure, the amount of the alkene (used in excess), and the (optional) presence of ethylene. In any case, the 1,4-hydrogenation, catalyzed by 1,2-di­methoxybenzene-Cr(CO)3, proceeds stereospecifically to yield exclusively the E-products from both the E- and Z-1,3-diene intermediates obtained by metathesis. A rather broad scope and functional group compatibility of the method is demonstrated by means of 15 examples.

Chiral Phosphine–Phosphite Ligands in Asymmetric Gold Catalysis: Highly Enantioselective Synthesis of Furo[3,4‐d]‐Tetrahydropyridazine Derivatives through [3+3]‐Cycloaddition

Q. Du, J.-M. Neudoerfl, H.-G. Schmalz, Chem. - Eur. J. 2018, 24, 2379-2383. 10.1002/chem.201800042


The AuI‐catalyzed reaction of 2‐(1‐alkynyl)‐2‐alken‐1‐ones with azomethine imines regio‐ and diastereoselectively affords furo[3,4‐d]tetrahydropyridazines in a tandem cyclization/intermolecular [3+3]‐cycloaddition process under mild conditions. By employing a chiral gold catalyst (prepared in situ from a Taddol‐derived phosphine‐phosphite ligand, Me2SAuCl, and AgOTf) high yields and enantioselectivities (up to 94 % yield, up to 96 % ee) are obtained. The method provides an efficient modular route to substituted heterotricyclic furan derivatives and can be easily scaled up (using catalyst loads of only 0.15 mol %).

Synthetic Indolactam V Analogues as Inhibitors of PAR2‐Induced Calcium Mobilization in Triple‐Negative Breast Cancer Cells

J. Stein, S. Stahn, J.-M. Neudoerfl, J. Sperlich, H.-G. Schmalz, N. Teusch, ChemMedChem 2018, 13, 147-154. 10.1002/cmdc.201700640


Human proteinase‐activated receptor 2 (PAR2), a transmembrane G‐protein‐coupled receptor (GPCR), is an attractive target for a novel anticancer therapy, as it plays a critical role in cell migration and invasion. Selective PAR2 inhibitors therefore have potential as anti‐metastatic drugs. Knowing that the natural product teleocidin A2 is able to inhibit PAR2 in tumor cells, the goal of the present study was to elaborate structure–activity relationships and to identify potent PAR2 inhibitors with lower activity against the adverse target, protein kinase C (PKC). For this purpose, an efficient gram‐scale total synthesis of indolactam V (i.e., the parent structure of all teleocidins) was developed, and a library of derivatives was prepared. Some compounds were indeed found to exhibit high potency as PAR2 inhibitors at low nanomolar concentrations with improved selectivity (relative to teleocidin A2). The pseudopeptidic fragment bridging the C3 and C4 positions of the indole core proved to be essential for target binding, whereas activity and target selectivity depends on the substituents at N1 or C7. This study revealed novel derivatives that show high efficacy in PAR2 antagonism combined with increased selectivity.

Design and Synthesis of Building Blocks for PPII‐Helix Secondary‐Structure Mimetics: A Stereoselective Entry to 4‐Substituted 5‐Vinylprolines

S. Chiha, A. Soicke, M. Barone, M. Mueller, J. Bruns, R. Opitz, J.-M. Neudoerfl, R. Kuehne, H.-G. Schmalz, Eur. J. Org. Chem. 2018, 2018, 455-460. 10.1002/ejoc.201701584


In the course of our studies towards the synthesis of proline‐based secondary‐structure mimetics, we developed a straightforward methodology for the diastereoselective preparation of 4‐alkyl‐5‐vinyl‐substituted proline derivatives. Starting from N‐Boc‐protected tert‐butyl pyroglutamate, α‐alkylation, lactam reduction and acid‐catalyzed methanolysis afforded 4‐alkyl‐5‐methoxyproline derivatives. After BF3‐induced formation of an N‐acyl‐iminium intermediate, the introduction of the 5‐vinyl side chain was achieved with high diastereoselectivity by using vinylmagnesium bromide in the presence of AlCl3 or CuBr·SMe2 to afford either the cis‐ or the trans‐product, respectively. The utility of the method was demonstrated in the rapid and efficient construction of new diproline mimetics rigidified in a polyproline‐type II helix (PPII) conformation.

Methyl Fumarate‐Derived Iron Carbonyl Complexes (FumET‐CORMs) as Powerful Anti‐inflammatory Agents

B. Bauer, A.-L. Goederz, H. Braumueller, J. M. Neudoerfl, M. Roecken, T. Wieder, H.-G. Schmalz, ChemMedChem 2017, 12, 1927-1930. 10.1002/cmdc.201700488


Autoimmune diseases are characterized by dendritic cell (DC)‐driven activation of pro‐inflammatory T cell responses. Therapeutic options for these severe diseases comprise small molecules such as dimethyl fumarate, or “gasotransmitters” such as CO. Herein we describe the synthesis of bifunctional enzyme‐triggered CO‐releasing molecules (ET‐CORMs) that allow the simultaneous intracellular release of both CO and methyl fumarate. Using bone‐marrow‐derived DCs the impressive therapeutic potential of these methyl fumarate‐derived compounds (FumET‐CORMs) is demonstrated by strong inhibition of lipopolysaccharide‐induced pro‐inflammatory signaling pathways and blockade of downstream interleukin‐12 or ‐23 production. The data also show that FumET‐CORMs are able to transform DCs into an anti‐inflammatory phenotype. Thus, these novel compounds have great clinical potential, for example, for the treatment of psoriasis or other inflammatory conditions of the skin.

Ergothioneine stands out from hercynine in the reaction with singlet oxygen: Resistance to glutathione and TRIS in the generation of specific products indicates high reactivity

C. Stoffels, M. Oumari, A. Perrou, A. Termath, W. Schlundt, H.-G. Schmalz, M. Schaefer, V. Wewer, S. Metzger, E. Schoemig, D. Gruendemann, Free Radical Biol. Med. 2017, 113, 385-394. 10.1016/j.freeradbiomed.2017.10.372


The candidate vitamin ergothioneine (ET), an imidazole-2-thione derivative of histidinebetaine, is generally considered an antioxidant. However, the precise physiological role of ET is still unresolved. Here, we investigated in vitro the hypothesis that ET serves specifically to eradicate noxious singlet oxygen (1O2). Pure 1O2 was generated by thermolysis at 37 °C of N,N'-di(2,3-dihydroxypropyl)-1,4-naphthalenedipropanamide 1,4-endoperoxide (DHPNO2). Assays of DHPNO2 with ET or hercynine (= ET minus sulfur) at pH 7.4 were analyzed by LC-MS in full scan mode to detect products. Based on accurate mass and product ion scan data, several products were identified and then quantitated as a function of time by selected reaction monitoring. All products of hercynine contained, after a [4+2] cycloaddition of 1O2, a carbonyl at position 2 of the imidazole ring. By contrast, because of the doubly bonded sulfur, we infer from the products of ET as the initial intermediates a 4,5-dioxetane (after [2+2] cycloaddition) and hydroperoxides at position 4 and 5 (after Schenck ene reactions). The generation of single products from ET, but not from hercynine, was fully resistant to a large excess of tris(hydroxymethyl)aminomethane (TRIS) or glutathione (GSH). This suggests that 1O2 markedly favors ET over GSH (at least 50-fold) and TRIS (at least 250-fold) for the initial reaction. Loss of ET was almost abolished in 5 mM GSH, but not in 25 mM TRIS. Regeneration of ET seems feasible, since some ET products – by contrast to hercynine products - decomposed easily in the MS collision cell to become aromatic again.

New Colchicine-Derived Triazoles and Their Influence on Cytotoxicity and Microtubule Morphology

P. Thomopoulou, J. Sachs, N. Teusch, A. Mariappan, J. Gopalakrishnan, H.-G. Schmalz, ACS Med. Chem. Lett. 2016, 7, 188-191. 10.1021/acsmedchemlett.5b00418


A series of new colchicinoids with a variable triazole unit at C-7 was synthesized through Cu(I)-catalyzed 1,3-dipolar cycloaddition (click-chemistry) of a colchicine-derived azide with various alkynes and the cytotoxicity against THP-1 and Jurkat cancer cell lines was used for structural optimization. Three particularly active compounds (IC50 ≤ 5 nM) were additionally investigated with respect to their efficacy against relevant solid tumor cell lines (HeLa, A549, and SK MES 1). Besides distorting the microtubule morphology by tubulin depolymerization, one compound also exhibited a pronounced centrosome declustering effect in triple negative breast cancer cells (MDA-MB-231) and nonsmall cell lung cancer cells (H1975).




[1]       An Atom-Economic and Stereospecific Access to Trisubstituted Olefins through Enyne Cross Metathesis Followed by 1,4-Hydrogenation, F. Ratsch, H. G. Schmalz, Synlett 201829, 785-792. 10.1055/s-0036-1591528


[2]       Chiral Phosphine-Phosphite Ligands in Asymmetric Gold Catalysis: Highly Enantioselective Synthesis of Furo 3,4-d -Tetrahydropyridazine Derivatives through 3+3 -Cycloaddition, Q. W. Du, J. M. Neudorfl, H. G. Schmalz, Chemistry-a European Journal 201824, 2379-2383. 10.1002/chem.201800042


[3]       Design and Synthesis of Building Blocks for PPII-Helix Secondary-Structure Mimetics: A Stereoselective Entry to 4-Substituted 5-Vinylprolines, S. Chiha, A. Soicke, M. Barone, M. Muller, J. Bruns, R. Opitz, J. M. Neudorfl, R. Kuhne, H. G. Schmalz, European Journal of Organic Chemistry 2018, 455-460. 10.1002/ejoc.201701584


[4]       Synthetic Indolactam V Analogues as Inhibitors of PAR2-Induced Calcium Mobilization in Triple-Negative Breast Cancer Cells, J. Stein, S. Stahn, J. M. Neudorfl, J. Sperlich, H. G. Schmalz, N. Teusch, Chemmedchem 201813, 147-154. 10.1002/cmdc.201700640


[5]       Methyl Fumarate-Derived Iron Carbonyl Complexes (FumET-CORMs) as Powerful Anti-inflammatory Agents, B. Bauer, A. L. Goderz, H. Braumuller, J. M. Neudorfl, M. Rocken, T. Wieder, H. G. Schmalz, Chemmedchem 201712, 1927-1930. 10.1002/cmdc.201700488


[6]       Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids, E. S. Shchegravina, A. A. Maleev, S. K. Ignatov, I. A. Gracheva, A. Stein, H. G. Schmalz, A. E. Gavryushin, A. A. Zubareva, E. V. Svirshchevskaya, A. Y. Fedorov, European Journal of Medicinal Chemistry 2017141, 51-60. 10.1016/j.ejmech.2017.09.055


[7]       Ergothioneine stands out from hercynine in the reaction with singlet oxygen: Resistance to glutathione and TRIS in the generation of specific products indicates high reactivity, C. Stoffels, M. Oumari, A. Perrou, A. Termath, W. Schlundt, H. G. Schmalz, M. Schafer, V. Wewer, S. Metzger, E. Schomig, D. Grundemann, Free Radical Biology and Medicine 2017113, 385-394. 10.1016/j.freeradbiomed.2017.10.372


[8]       Tandem Hydroalumination/Cu-Catalyzed Asymmetric Vinyl Metalation as a New Access to Enantioenriched Vinylcyclopropane Derivatives, D. S. Muller, V. Werner, S. Akyol, H. G. Schmalz, I. Marek, Organic Letters 201719, 3970-3973. 10.1021/acs.orglett.7b01661


[9]       Organocatalyzed Synthesis of Oleochemical Carbonates from CO2 and Renewables, H. Buttner, J. Steinbauer, C. Wulf, M. Dindaroglu, H. G. Schmalz, T. Werner, Chemsuschem 201710, 1076-1079. 10.1002/cssc.201601163


[10]     Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids, I. A. Gracheva, I. V. Voitovich, V. I. Faerman, N. S. Sitnikov, E. V. Myrsikova, H. G. Schmalz, E. V. Svirshevskaya, A. Y. Fedorov, European Journal of Medicinal Chemistry 2017126, 432-443. 10.1016/j.ejmech.2016.11.020


[11]     Synthesis of Nonracemic Pyrrolo-allocolchicinoids Exhibiting Potent Cytotoxic Activity, E. S. Shchegravina, D. I. Knyazev, I. P. Beletskaya, E. V. Svirshchevskaya, H. G. Schmalz, A. Y. Fedorov, European Journal of Organic Chemistry 2016, 5620-5623. 10.1002/ejoc.201601069


[12]     Prevention of colitis by controlled oral drug delivery of carbon monoxide, C. Steiger, K. Uchiyama, T. Takagi, K. Mizushima, Y. Higashimura, M. Gutmann, C. Hermann, S. Botov, H. G. Schmalz, Y. Naito, L. Meinel, Journal of Controlled Release 2016239, 128-136. 10.1016/j.jconrel.2016.08.030


[13]     A fast and simple LC-MS-based characterization of the flavonoid biosynthesis pathway for few seed(ling)s, B. Jaegle, M. K. Uroic, X. Holtkotte, C. Lucas, A. O. Termath, H. G. Schmalz, M. Bucher, U. Hoecker, M. Hulskamp, A. Schrader, Bmc Plant Biology 201616. 10.1186/s12870-016-0880-7


[14]     Synthesis of New Sulfur-Containing Derivatives of Furanoallocolchicinoids, Y. A. Gracheva, H. G. Schmalz, E. V. Svirshchevskaya, A. Y. Fedorov, Russian Journal of Organic Chemistry 201652, 1137-1142. 10.1134/s1070428016080078


[15]     Low-Pressure Cobalt-Catalyzed Enantioselective Hydrovinylation of Vinylarenes, S. Movahhed, J. Westphal, M. Dindaroglu, A. Falk, H. G. Schmalz, Chemistry-a European Journal 201622, 7381-7384. 10.1002/chem.201601283


[16]     Total Synthesis of the Antiviral Natural Product Houttuynoid B, T. Kerl, F. Berger, H. G. Schmalz, Chemistry-a European Journal 201622, 2935-2938. 10.1002/chem.201505118


[17]     New Colchicine-Derived Triazoles and Their Influence on Cytotoxicity and Microtubule Morphology, P. Thomopoulou, J. Sachs, N. Teusch, A. Mariappan, J. Gopalakrishnan, H. G. Schmalz, Acs Medicinal Chemistry Letters 20167, 188-191. 10.1021/acsmedchemlett.5b00418


[18]     Synthesis of Chlorin-(Arylamino)quinazoline Hybrids as Models for Multifunctional Drug Development, A. V. Nyuchev, V. F. Otvagin, A. E. Gavryushin, Y. I. Romanenko, O. I. Koifman, D. V. Belykh, H. G. Schmalz, A. Y. Fedorov, Synthesis-Stuttgart 201547, 3717-3726. 10.1055/s-0034-1378876


[19]     Design, Synthesis, and Functional Evaluation of CO-Releasing Molecules Triggered by Penicillin G Amidase as a Model Protease, N. S. Sitnikov, Y. C. Li, D. F. Zhang, B. Yard, H. G. Schmalz, Angewandte Chemie-International Edition 2015,54, 12314-12318. 10.1002/anie.201502445


[20]     Enantioselective Nickel-Catalyzed Hydrocyanation using Chiral Phosphine-Phosphite Ligands: Recent Improvements and Insights, A. Falk, A. Cavalieri, G. S. Nichol, D. Vogt, H. G. Schmalz, Advanced Synthesis & Catalysis 2015357, 3317-3320. 10.1002/adsc.201500644


[21]     Synthesis of Diverse 6-Oxa-allocolchicinoids by a Suzuki-Miyaura Coupling, Acid-Catalyzed Intramolecular Transacetalization Strategy, D. B. Yadav, L. Taleli, A. E. van der Westhuyzen, M. A. Fernandes, M. Dragoun, A. Prokop, H. G. Schmalz, C. B. de Koning, W. A. L. van Otterlo, European Journal of Organic Chemistry 2015, 5167-5182. 10.1002/ejoc.201500573


[22]     Organometallic nucleosides induce non-classical leukemic cell death that is mitochondrial-ROS dependent and facilitated by TCL1-oncogene burden, C. Prinz, E. Vasyutina, G. Lohmann, A. Schrader, S. Romanski, C. Hirschhauser, P. Mayer, C. Frias, C. D. Herling, M. Hallek, H. G. Schmalz, A. Prokop, D. Mougiakakos, M. Herling, Molecular Cancer201514. 10.1186/s12943-015-0378-1


[23]     Synthesis and antitumor activity of 7-(triazol-1-yl)pyrroloallocolchicine derivatives, N. S. Sitnikov, A. V. Sintsov, E. S. Shchegravina, A. Prokop, H. G. Schmalz, V. V. Fokin, A. Y. Fedorov, Russian Chemical Bulletin 201564, 1362-1368. 10.1007/s11172-015-1018-z


[24]     Biomimetic Synthesis of Isoindolinones Related to the Marilines, D. Augner, H. G. Schmalz, Synlett 201526, 1395-1397. 10.1055/s-0034-1380700


[25]     Design and Stereoselective Synthesis of ProM-2: A Spirocyclic Diproline Mimetic with Polyproline Type II (PPII) Helix Conformation, C. Reuter, R. Opitz, A. Soicke, S. Dohmen, M. Barone, S. Chiha, M. T. Klein, J. M. Neudorfl, R. Kuhne, H. G. Schmalz, Chemistry-a European Journal 201521, 8464-8470. 10.1002/chem.201406493


[26]     A modular toolkit to inhibit proline-rich motif-mediated protein-protein interactions, R. Opitz, M. Muller, C. Reuter, M. Barone, A. Soicke, Y. Roske, K. Piotukh, P. Huy, M. Beerbaum, B. Wiesner, M. Beyermann, P. Schmieder, C. Freund, R. Volkmer, H. Oschkinat, H. G. Schmalz, R. Kuhne, Proceedings of the National Academy of Sciences of the United States of America 2015112, 5011-5016. 10.1073/pnas.1422054112


[27]     Synthesis and Biological Evaluation of Furanoallocolchicinoids, Y. V. Voitovich, E. S. Shegravina, N. S. Sitnikov, V. I. Faerman, V. V. Fokin, H. G. Schmalz, S. Combes, D. Allegro, P. Barbier, I. P. Beletskaya, E. V. Svirshchevskaya, A. Y. Fedorov, Journal of Medicinal Chemistry 201558, 692-704. 10.1021/jm501678w


[28]     Synthesis of indole-derived allocolchicine congeners exhibiting pronounced anti-proliferative and apoptosis-inducing properties, N. S. Sitnikov, A. V. Sinzov, D. Allegro, P. Barbier, S. Combes, L. A. Onambele, A. Prokop, H. G. Schmalz, A. Y. Fedorov, Medchemcomm20156, 2158-2162. 10.1039/c5md00320b


[29]     Individual steps of the Mizoroki-Heck reaction and intrinsic reactivity of intermediate organopalladium complexes studied in the gas phase, L. Fiebig, J. Held, H. G. Schmalz, M. Schafer, European Journal of Mass Spectrometry 2015,21, 623-633. 10.1255/ejms.1310


[30]     Stereoselective Synthesis of Tricyclic Diproline Analogues that Mimic a PPII Helix: Structural Consequences of Ring-Size Variation, A. Soicke, C. Reuter, M. Winter, J. M. Neudorfl, N. Schlorer, R. Kuhne, H. G. Schmalz, European Journal of Organic Chemistry 2014, 6467-6480. 10.1002/ejoc.201402737


[31]     Synthesis of Indole-Derived Allocolchicine Congeners through Pd-Catalyzed Intramolecular C-H Arylation Reaction, N. S. Sitnikov, A. S. Kokisheva, G. K. Fukin, J. M. Neudorfl, H. Sutorius, A. Prokop, V. V. Fokin, H. G. Schmalz, A. Y. Fedorov, European Journal of Organic Chemistry 2014, 6481-6492. 10.1002/ejoc.201402850


[32]     Total Synthesis of (R, R, R)-alpha-Tocopherol Through Asymmetric Cu-Catalyzed 1,4-Addition, A. O. Termath, H. Sebode, W. Schlundt, R. T. Stemmler, T. Netscher, W. Bonrath, H. G. Schmalz, Chemistry-a European Journal 2014,20, 12051-12055. 10.1002/chem.201404379


[33]     Synthesis of C-2-Symmetric Bisphosphine Ligands from Tartaric Acid, and Their Performance in the Pd-Catalyzed Asymmetric O-Allylation of a Phenol, M. Dindaroglu, A. Dincer, H. G. Schmalz, European Journal of Organic Chemistry 2014, 4315-4326. 10.1002/ejoc.201402326


[34]     Total Synthesis of (2RS)-alpha-Tocopherol through Ni-Catalyzed 1,4-Addition to a Chromenone Intermediate, A. O. Termath, J. Velder, R. T. Stemmler, T. Netscher, W. Bonrath, H. G. Schmalz, European Journal of Organic Chemistry 20142014, 3337-3340. 10.1002/ejoc.201402240


[35]     Stereoselective Synthesis of Proline- Derived Dipeptide Scaffolds ( ProM-3 and ProM-7) Rigidified in a PPII Helix Conformation, C. Reuter, M. Kleczka, S. de Mazancourt, J. M. Neudorfl, R. Kuhne, H. G. Schmalz, European Journal of Organic Chemistry 20142014, 2664-2667. 10.1002/ejoc.201301875


[36]     Aryl-Phenyl Scrambling in Intermediate Organopalladium Complexes: A Gas-Phase Study of the Mizoroki-Heck Reaction, L. Fiebig, N. Schlorer, H. G. Schmalz, M. Schafer, Chemistry-a European Journal 201420, 4906-4910. 10.1002/chem.201400115


[37]     Different design of enzyme-triggered CO-releasing molecules (ET-CORMs) reveals quantitative differences in biological activities in terms of toxicity and inflammation, E. Stamellou, D. Storz, S. Botov, E. Ntasis, J. Wedel, S. Sollazzo, B. K. Kramer, W. van Son, M. Seelen, H. G. Schmalz, A. Schmidt, M. Hafner, B. A. Yard, Redox Biology 20142, 739-748. 10.1016/j.redox.2014.06.002


[38]     New modular manganese(I) tricarbonyl complexes as PhotoCORMs: in vitro detection of photoinduced carbon monoxide release using COP-1 as a fluorogenic switch-on probe, S. Pai, M. Hafftlang, G. Atongo, C. Nagel, J. Niesel, S. Botov, H. G. Schmalz, B. Yard, U. Schatzschneider, Dalton Transactions 2014,43, 8664-8678. 10.1039/c4dt00254g


[39]     Asymmetric catalytic arylation of ethyl glyoxylate using organoboron reagents and Rh(I)-phosphane and phosphane-phosphite catalysts, C. S. Marques, M. Dindaroglu, H. G. Schmalz, A. J. Burke, Rsc Advances 20144, 6035-6041. 10.1039/c3ra47000h


[40]     Enzyme-triggered CO-releasing molecules (ET-CORMs): Evaluation of biological activity in relation to their structure, S. Romanski, E. Stamellou, J. T. Jaraba, D. Storz, B. K. Kramer, M. Hafner, S. Amslinger, H. G. Schmalz, B. A. Yard, Free Radical Biology and Medicine 201365, 78-88. 10.1016/j.freeradbiomed.2013.06.014


[41]     Cobalt Catalysis in the Gas Phase: Experimental Characterization of Cobalt(I) Complexes as Intermediates in Regioselective Diels-Alder Reactions, L. Fiebig, J. Kuttner, G. Hilt, M. C. Schwarzer, G. Frenking, H. G. Schmalz, M. Schafer, Journal of Organic Chemistry 201378, 10485-10493. 10.1021/jo402001g


[42]     Nucleoside Analogues with a 1,3-Diene-Fe(CO)(3) Substructure: Stereoselective Synthesis, Configurational Assignment, and Apoptosis-Inducing Activity, C. Hirschhauser, J. Velcicky, D. Schlawe, E. Hessler, A. Majdalani, J. M. Neudorfl, A. Prokop, T. Wieder, H. G. Schmalz, Chemistry-a European Journal 201319, 13017-13029. 10.1002/chem.201301672


[43]     Efficient -Helix Induction in a Linear Peptide Chain by N-Capping with a ridged-tricyclic Diproline Analogue, V. Hack, C. Reuter, R. Opitz, P. Schmieder, M. Beyermann, J. M. Neudorfl, R. Kuhne, H. G. Schmalz, Angewandte Chemie-International Edition 201352, 9539-9543. 10.1002/anie.201302014


[44]     Lipophilic prodrugs of a triazole-containing colchicine analogue in liposomes: Biological effects on human tumor cells, N. R. Kuznetsova, E. V. Svirshchevskaya, N. S. Sitnikov, L. Abodo, H. Sutorius, J. Zapke, J. Velder, P. Thomopoulou, H. Oschkinat, A. Prokop, H. G. Schmalz, A. Y. Fedorov, E. L. Vodovozova, Russian Journal of Bioorganic Chemistry 201339, 543-552. 10.1134/s1068162013050105


[45]     On the Antibiotic and Antifungal Activity of Pestalone, Pestalachloride A, and Structurally Related Compounds, D. Augner, O. Krut, N. Slavov, D. C. Gerbino, H. G. Sahl, J. Benting, C. F. Nising, S. Hillebrand, M. Kronke, H. G. Schmalz, Journal of Natural Products 201376, 1519-1522. 10.1021/np400301d


[46]     Synthesis and Performance of Acyloxy-diene-Fe(CO)(3) Complexes with Variable Chain Lengths as Enzyme-Triggered Carbon Monoxide-Releasing Molecules, S. Botov, E. Stamellou, S. Romanski, M. Guttentag, R. Alberto, J. M. Neudorfl, B. Yard, H. G. Schmalz, Organometallics 201332, 3587-3594. 10.1021/om301733h


[47]     TARTROL-derived chiral phosphine-phosphite ligands and their performance in enantioselective Cu-catalyzed 1,4-addition reactions, M. Dindaroglu, S. Akyol, H. Simsir, J. M. Neudorfl, A. Burke, H. G. Schmalz, Tetrahedron-Asymmetry 201324, 657-662. 10.1016/j.tetasy.2013.04.008


[48]     A Scalable Synthesis of Chiral Modular Phosphine-Phosphite Ligands, M. Dindaroglu, A. Falk, H. G. Schmalz, Synthesis-Stuttgart201345, 527-535. 10.1055/s-0032-1316847


[49]     Enantioselective Nickel-Catalyzed Hydrocyanation of Vinylarenes Using Chiral Phosphine-Phosphite Ligands and TMS-CN as a Source of HCN, A. Falk, A. L. Goderz, H. G. Schmalz, Angewandte Chemie-International Edition 2013,52, 1576-1580. 10.1002/anie.201208082


[50]     An Enantioselective Total Synthesis of Helioporins C and E, W. Lolsberg, S. Werle, J. M. Neudorfl, H. G. Schmalz, Organic Letters 201214, 5996-5999. 10.1021/ol302898h


[51]     Ligand Control of the Cobalt-Catalysed 1,4-Hydrovinylation Reaction, M. Arndt, M. Dindaroglu, H. G. Schmalz, G. Hilt, Synthesis-Stuttgart 2012,44, 3534-3542. 10.1055/s-0032-1316796


[52]     TADDOL-Based Phosphane-Phosphite Ligands in Enantioselective Cu-Catalyzed Grignard 1,4-Additions Followed by Mannich-Type Alkylations, M. Drusan, W. Lolsberg, A. Skvorcova, H. G. Schmalz, R. Sebesta, European Journal of Organic Chemistry 2012, 6285-6290. 10.1002/ejoc.201200729


[53]     Hydrophenalene-Cr(CO)(3) complexes as anti-inflammatory agents based on specific inhibition of NOD2 signalling: a SAR study, A. Saiai, H. Bielig, J. Velder, J. M. Neudorfl, M. Menning, T. A. Kufer, H. G. Schmalz, Medchemcomm 20123, 1377-1385. 10.1039/c2md20221b


[54]     Total Synthesis of Indole-Derived Allocolchicine Analogues Exhibiting Strong Apoptosis-Inducing Activity, N. Sitnikov, J. Velder, L. Abodo, N. Cuvelier, J. Neudorfl, A. Prokop, G. Krause, A. Y. Fedorov, H. G. Schmalz, Chemistry-a European Journal 201218, 12096-12102. 10.1002/chem.201200083


[55]     Iron Dienylphosphate Tricarbonyl Complexes as Water-Soluble Enzyme-Triggered CO-Releasing Molecules (ET-CORMs), S. Romanski, H. Rucker, E. Stamellou, M. Guttentag, J. M. Neudorfl, R. Alberto, S. Amslinger, B. Yard, H. G. Schmalz, Organometallics 201231, 5800-5809. 10.1021/om300359a


[56]     Synthesis of Oxa-B-Ring Analogs of Colchicine through Rh-Catalyzed Intramolecular 5+2 Cycloaddition, A. O. Termath, S. Ritter, M. Konig, D. P. Kranz, J. M. Neudorfl, A. Prokop, H. G. Schmalz, European Journal of Organic Chemistry 2012, 4501-4507. 10.1002/ejoc.201200677


[57]     Synthesis of B-Ring-Modified Steroids through BF3-Promoted Rearrangement/Substitution of 6 beta-Hydroxy-5,19-cyclosteroids, D. P. Kranz, S. Chiha, A. M. Z. Greffen, J. M. Neudorfl, H. G. Schmalz, Organic Letters 201214, 3692-3695. 10.1021/ol301532w


[58]     Nucleophile- or Light-Induced Synthesis of 3-Substituted Phthalides from 2-Formylarylketones, D. C. Gerbino, D. Augner, N. Slavov, H. G. Schmalz, Organic Letters 201214, 2338-2341. 10.1021/ol300757m


[59]     Cu-Catalyzed Enantioselective 1,4-Additions of Aryl-Grignard Reagents to Cyclohexenone in the Presence of TADDOL-Derived Phosphane-Phosphite Ligands, Q. Naeemi, M. Dindaroglu, D. P. Kranz, J. Velder, H. G. Schmalz, European Journal of Organic Chemistry 2012, 1179-1185. 10.1002/ejoc.201101258


[60]     Acyloxybutadiene tricarbonyl iron complexes as enzyme-triggered CO-releasing molecules (ET-CORMs): a structure-activity relationship study, S. Romanski, B. Kraus, M. Guttentag, W. Schlundt, H. Rucker, A. Adler, J. M. Neudorfl, R. Alberto, S. Amslinger, H. G. Schmalz, Dalton Transactions 201241, 13862-13875. 10.1039/c2dt30662j


[61]     Molecular Oxygen as a Redox Catalyst in Intramolecular Photocycloadditions of Coumarins, D. P. Kranz, A. G. Griesbeck, R. Alle, R. Perez-Ruiz, J. M. Neudorfl, K. Meerholz, H. G. Schmalz, Angewandte Chemie-International Edition 201251, 6000-6004. 10.1002/anie.201201222


[62]     A novel conjugate of a cell-penetrating peptide and a ferrocenyl amino acid: a potential electrochemical sensor for living cells?, J. Hoyer, A. Hunold, H. G. Schmalz, I. Neundorf, Dalton Transactions 201241, 6396-6398. 10.1039/c2dt12211a


[63]     Gaining Absolute Control of the Regiochemistry in the Cobalt-Catalyzed 1,4-Hydrovinylation Reaction, M. Arndt, M. Dindaroglu, H. G. Schmalz, G. Hilt, Organic Letters 201113, 6236-6239. 10.1021/ol202696n


[64]     Rhodium-Catalyzed Enantioselective Intramolecular 4+2 Cycloaddition using a Chiral Phosphine-Phosphite Ligand: Importance of Microwave-Assisted Catalyst Conditioning, A. Falk, L. Fiebig, J. M. Neudorfl, A. Adler, H. G. Schmalz, Advanced Synthesis & Catalysis 2011353, 3357-3362. 10.1002/adsc.201100658


[65]     Heck coupling in the gas phase: Examination of the reaction mechanism by ion/molecule reactions and mass spectrometry, L. Fiebig, H. G. Schmalz, M. Schafer, International Journal of Mass Spectrometry 2011308, 307-310. 10.1016/j.ijms.2011.07.013


[66]     (RS)-Tricarbonyl(eta(4)-1,3-diacetoxy-5,5-dimethylcyclohexa-1,3-diene) iron(0), S. Romanski, J. M. Neudorfl, H. G. Schmalz, Acta Crystallographica Section E-Structure Reports Online 201167, M1530-+. 10.1107/s1600536811041298


[67]     Enantioselective Access to 3-Methylene-1H-indanol through Asymmetric Domino Allylstannylation-Heck Reaction, J. Schutte, S. T. Ye, H. G. Schmalz,Synlett 2011, 2725-2729. 10.1055/s-0031-1289539


[68]     N-Capping of Primary Amines with 2-Acyl-benzaldehydes To Give Isoindolinones, D. Augner, D. C. Gerbino, N. Slavov, J. M. Neudorfl, H. G. Schmalz, Organic Letters 201113, 5374-5377. 10.1021/ol202271k


[69]     Exercises in Pyrrolidine Chemistry: Gram Scale Synthesis of a Pro-Pro Dipeptide Mimetic with a Polyproline Type II Helix Conformation, C. Reuter, P. Huy, J. M. Neudorfl, R. Kuhne, H. G. Schmalz, Chemistry-a European Journal 2011,17, 12037-12044. 10.1002/chem.201101704


[70]     Metal-Free Intramolecular Carbonyl-Olefin Metathesis of ortho-Prenylaryl Ketones, A. Soicke, N. Slavov, J. M. Neudorfl, H. G. Schmalz, Synlett 2011, 2487-2490. 10.1055/s-0030-1260320


[71]     Stereoselective Synthesis and Biological Evaluation of Ferrocene-Containing 5-Hydroxyeicosatetraenoic Acid Analogues, N. Kausch-Busies, J. M. Neudorfl, P. Wefelmeier, A. Prokop, H. Kuhn, H. G. Schmalz, European Journal of Organic Chemistry 2011, 4634-4644. 10.1002/ejoc.201100003


[72]     Palladium-Catalyzed Cyanomethylation of Aryl Halides through Domino Suzuki Coupling-Isoxazole Fragmentation, J. Velcicky, A. Soicke, R. Steiner, H. G. Schmalz, Journal of the American Chemical Society 2011133, 6948-6951. 10.1021/ja201743j


[73]     Sn(OTf)(2) as an Effective Lewis Acid in Reactions of Cyclopropyl Ketones with Acetic Anhydride: Application in the Synthesis of a 19-Nor-B-homo Steroid, D. P. Kranz, A. M. Z. Greffen, S. El Sheikh, J. M. Neudorfl, H. G. Schmalz, European Journal of Organic Chemistry2011, 2860-2866. 10.1002/ejoc.201100020


[74]     Chiral phosphine-phosphite ligands in the enantioselective 1,4-addition of Grignard reagents to alpha,beta-unsaturated carbonyl compounds, Q. Naeemi, T. Robert, D. P. Kranz, J. Velder, H. G. Schmalz, Tetrahedron-Asymmetry 2011,22, 887-892. 10.1016/j.tetasy.2011.04.018


[75]     Iron containing anti-tumoral agents: unexpected apoptosis-inducing activity of a ferrocene amino acid derivative, B. Kater, A. Hunold, H. G. Schmalz, L. Kater, B. Bonitzki, P. Jesse, A. Prokop, Journal of Cancer Research and Clinical Oncology 2011137, 639-649. 10.1007/s00432-010-0924-6


[76]     A CONVENIENT ENTRY TO NEW C-7-MODIFIED COLCHICINOIDS THROUGH AZIDE ALKYNE 3+2 CYCLOADDITION: APPLICATION OF RING-CONTRACTIVE REARRANGEMENTS, N. Nicolaus, J. Reball, N. Sitnikov, J. Velder, A. Termath, A. Y. Fedorov, H. G. Schmalz, Heterocycles 201182, 1585-+. 10.3987/com-10-s(e)117


[77]     Practical One-Pot Double Functionalizations of Proline, P. Huy, H. G. Schmalz, Synthesis-Stuttgart 2011, 954-960. 10.1055/s-0030-1258428


[78]     Total Synthesis of cyclo-Mumbaistatin Analogues through Anionic Homo-Fries Rearrangement, S. Neufeind, N. Hulsken, J. M. Neudorfl, N. Schlorer, H. G. Schmalz, Chemistry-a European Journal 201117, 2633-2641. 10.1002/chem.201003166


[79]     Synthesis and First Biological Evaluation of an Iron-Containing HETE Analogue, N. Kausch-Busies, B. Kater, J. M. Neudorfl, A. Prokop, H. G. Schmalz, European Journal of Organic Chemistry 2011, 1133-1139. 10.1002/ejoc.201001445


[80]     A Practical Synthesis of Trans-3-Substituted Proline Derivatives through 1,4-Addition, P. Huy, J. M. Neudorfl, H. G. Schmalz, Organic Letters 201113, 216-219. 10.1021/ol102613z


[81]     Acyloxybutadiene Iron Tricarbonyl Complexes as Enzyme-Triggered CO-Releasing Molecules (ET-CORMs), S. Romanski, B. Kraus, U. Schatzschneider, J. M. Neudorfl, S. Amslinger, H. G. Schmalz, Angewandte Chemie-International Edition 201150, 2392-2396. 10.1002/anie.201006598


[82]     Cobalt-Catalyzed 1,4-Hydrobutadienylation of 1-Aryl-1,3-dienes with 2,3-Dimethyl-1,3-butadiene, M. A. Bohn, A. Schmidt, G. Hilt, M. Dindaroglu, H. G. Schmalz, Angewandte Chemie-International Edition 2011,50, 9689-9693. 10.1002/anie.201103613


[83]     Paraoxonase-1 is a major determinant of clopidogrel efficacy, H. J. Bouman, E. Schomig, J. W. van Werkum, J. Velder, C. M. Hackeng, C. Hirschhauser, C. Waldmann, H. G. Schmalz, J. M. ten Berg, D. Taubert, Nature Medicine 201117, 110-U287. 10.1038/nm.2281


[84]     Anti-inflammatory Arene-Chromium Complexes Acting as Specific Inhibitors of NOD2 Signalling, H. Bielig, J. Velder, A. Saiai, M. Menning, S. Meemboor, W. Kalka-Moll, M. Kronke, H. G. Schmalz, T. A. Kufer, Chemmedchem 20105, 2065-2071. 10.1002/cmdc.201000320


[85]     Phenol-derived chiral phosphine-phosphite ligands in the rhodium-catalyzed enantioselective hydrogenation of functionalized olefins, T. Robert, Z. Abiri, A. J. Sandee, H. G. Schmalz, J. N. H. Reek, Tetrahedron-Asymmetry 201021, 2671-2674. 10.1016/j.tetasy.2010.10.026


[86]     Synthesis of Novel Allocolchicine Analogues with a Pyridine C-Ring through Intermolecular Vollhardt Diyne-Nitrile Cyclotrimerization, N. Nicolaus, H. G. Schmalz, Synlett 2010, 2071-2074. 10.1055/s-0030-1258512


[87]     Enantioselective Copper-Catalysed Allylic Alkylation of Cinnamyl Chlorides by Grignard Reagents using Chiral Phosphine-Phosphite Ligands, W. Loelsberg, S. Ye, H. G. Schmalz, Advanced Synthesis & Catalysis 2010352, 2023-2031. 10.1002/adsc.201000213


[88]     Stereospecificity of the Au(I)-catalyzed reaction of 1-alkynyl-bicyclo 4.1.0 -heptan-2-ones with nucleophiles, S. Labsch, S. Ye, A. Adler, J. M. Neudorfl, H. G. Schmalz, Tetrahedron-Asymmetry201021, 1745-1751. 10.1016/j.tetasy.2010.05.019


[89]     Azides Derived from Colchicine and their Use in Library Synthesis: a Practical Entry to New Bioactive Derivatives of an Old Natural Drug, N. Nicolaus, J. Zapke, P. Riesterer, J. M. Neudorfl, A. Prokop, H. Oschkinat, H. G. Schmalz, Chemmedchem 20105, 661-665. 10.1002/cmdc.201000063


[90]     Potassium (1-methoxycarbonyl-2-methylprop-2-en-2-ylidene)azinate, C. Reuter, J. M. Neudorfl, H. G. Schmalz, Acta Crystallographica Section E-Structure Reports Online 201066, M461-U1150. 10.1107/s1600536810010159


[91]     New caspase-independent but ROS-dependent apoptosis pathways are targeted in melanoma cells by an iron-containing cytosine analogue, J. C. Franke, M. Plotz, A. Prokop, C. C. Geilen, H. G. Schmalz, J. Eberle, Biochemical Pharmacology 2010,79, 575-586. 10.1016/j.bcp.2009.09.022


[92]     A Scalable Synthesis of (+/-)-2-Oxoclopidogrel, J. Velder, C. Hirschhauser, C. Waldmann, D. Taubert, H. J. Bouman, H. G. Schmalz, Synlett 2010, 467-469. 10.1055/s-0029-1219177


[93]     Asymmetric Hydroformylation Using Taddol-Based Chiral Phosphine-Phosphite Ligands, T. Robert, Z. Abiri, J. Wassenaar, A. J. Sandee, S. Romanski, J. M. Neudorfl, H. G. Schmalz, J. N. H. Reek, Organometallics 201029, 478-483. 10.1021/om9009735


[94]     Addressing Protein-Protein Interactions with Small Molecules: A Pro-Pro Dipeptide Mimic with a PPII Helix Conformation as a Module for the Synthesis of PRD-Binding Ligands, J. Zaminer, C. Brockmann, P. Huy, R. Opitz, C. Reuter, M. Beyermann, C. Freund, M. Muller, H. Oschkinat, R. Kuhne, H. G. Schmalz, Angewandte Chemie-International Edition 201049, 7111-7115. 10.1002/anie.201001739


[95]     Total Synthesis of the Marine Antibiotic Pestalone and its Surprisingly Facile Conversion into Pestalalactone and Pestalachloride A, N. Slavov, J. Cvengros, J. M. Neudorfl, H. G. Schmalz, Angewandte Chemie-International Edition 2010,49, 7588-7591. 10.1002/anie.201003755


[96]     trans-Ethylenedi-p-phenylene diacetate, S. Ritter, J. M. Neudorfl, J. Velder, H. G. Schmalz, Acta Crystallographica Section E-Crystallographic Communications 200965, O2229-U2693. 10.1107/s1600536809032620


[97]     trans-1,2-Bis(3,5-dimethoxyphenyl)ethene, S. Ritter, J. M. Neudorfl, J. Velder, H. G. Schmalz, Acta Crystallographica Section E-Structure Reports Online 200965, O2150-U1997. 10.1107/s160053680903116x


[98]     Stereoselective Synthesis of New Ferrocene-Derived Amino Acid Building Blocks, A. Hunold, I. Neundorf, P. James, J. Neudorfl, H. G. Schmalz, European Journal of Organic Chemistry 2009, 4429-4440. 10.1002/ejoc.200900552


[99]     Introduction of Allyl and Prenyl Side-Chains into Aromatic Systems by Suzuki Cross-Coupling Reactions, D. C. Gerbino, S. D. Mandolesi, H. G. Schmalz, J. C. Podesta, European Journal of Organic Chemistry 2009, 3964-3972. 10.1002/ejoc.200900234


[100]  A 2+2+2 -Cycloaddition Approach toward 6-Oxa-allocolchicinoids with Apoptosis-inducing Activity, N. Nicolaus, S. Strauss, J. M. Neudorfl, A. Prokop, H. G. Schmalz, Organic Letters 200911, 341-344. 10.1021/ol802542c


[101]  Electrophilic Activation of Benzaldehydes through ortho Palladation: One-Pot Synthesis of 3-Methylene-indan-1-ols through a Domino Allylstannylation/Heck Reaction under Neutral Conditions, J. Cvengros, J. Schutte, N. Schlorer, J. Neudorfl, H. G. Schmalz, Angewandte Chemie-International Edition 200948, 6148-6151. 10.1002/anie.200901837


[102]  Microwave-assisted cleavage of aryl methyl ethers with lithium thioethoxide (LiSEt), J. Cvengros, S. Neufeind, A. Becker, H. G. Schmalz, Synlett 2008, 1993-1998. 10.1055/s-2008-1077949


[103]  Modular synthesis of chiral phosphine-phosphite-ligands from phenolic precursors: A new approach to bidentate chelate ligands exploiting a P-O to P-C migration rearrangement, J. Velder, T. Robert, I. Weidner, J. M. Neudorfl, J. Lex, H. G. Schmalz, Advanced Synthesis & Catalysis 2008350, 1309-1315. 10.1002/adsc.200800146


[104]  Butyllithium-mediated coupling of aryl bromides with ketones under in-situ-quench (ISQ) conditions: An efficient one-step protocol applicable to microreactor technology, S. Goto, J. Velder, S. El Sheikh, Y. Sakamoto, M. Mitani, S. Elmas, A. Adler, A. Becker, J. M. Neudorfl, J. Lex, H. G. Schmalz, Synlett 2008, 1361-1365. 10.1055/s-2008-1072771


[105]  Enantioselective Cu-catalyzed 1,4-addition of Grignard reagents to cyclohexenone using Taddol-derived phosphine-phosphite ligands and 2-methyl-THF as a solvent, T. Robert, J. Velder, H. G. Schmalz, Angewandte Chemie-International Edition 200847, 7718-7721. 10.1002/anie.200803247


[106]  Synthesis of a mumbaistatin analogue through cross-coupling, D. Sucunza, D. Dembkowski, S. Neufeind, J. Velder, J. Lex, H. G. Schmalz, Synlett 2007, 2569-2573. 10.1055/s-2007-986652


[107]  Enantioselective Synthesis of a trans-7,8-Dimethoxycalamenene, S. Werle, T. Fey, J. M. Neudorfl, H. G. Schmalz, Organic Letters 20079, 3555-3558. 10.1021/ol071228v


[108]  Stereospecific side chain activation in Cyclobutadiene-Fe(CO)(3) chemistry: A theoretical and experimental study on the structure and configurational stability of cationic, radical and anionic intermediates, A. Pfletschinger, U. Schneider, J. Lex, H. G. Schmalz, European Journal of Organic Chemistry 2007, 3991-3998. 10.1002/ejoc.200700342


[109]  Synthesis of the core structure of the cyclocitrinols via SmI(2)-mediated fragmentation of a cyclopropane precursor, S. El Sheikh, A. M. Z. Greffen, J. Lex, J. M. Neudorfl, H. G. Schmalz, Synlett 2007, 1881-1884.10.1055/s-2007-984521


[110]  Stereoselective syntheses of the 2-isopropenyl-2,3-dihydrobenzofuran nucleus: Potential chiral building blocks for the syntheses of tremetone, hydroxytremetone, and rotenone, S. C. Pelly, S. Govender, M. A. Fernandes, H. G. Schmalz, C. B. de Koning, Journal of Organic Chemistry 200772, 2857-2864. 10.1021/jo062447h


[111]  Synthesis of 4-benzyliden-2-oxazolidinone derivatives via gold-catalyzed intramolecular hydroamination, S. Ritter, K. Hackeloer, H. G. Schmalz, Heterocycles 200774, 731-742

[112]  Gold-catalyzed cyclization of O-propargyl carbamates under mild conditions: A convenient access to 4-alkylidene-2-oxazolidinones, S. Ritter, Y. Horino, J. Lex, H. G. Schmalz, Synlett2006, 3309-3313. 10.1055/s-2006-951555


[113]  Gram-scale synthesis of pinusolide and evaluation of its antileukemic potential, E. E. Shults, J. Velder, H. G. Schmalz, S. V. Chernov, T. V. Rubalova, Y. V. Gatilov, G. Henze, G. A. Tolstikov, A. Prokop, Bioorganic & Medicinal Chemistry Letters200616, 4228-4232. 10.1016/j.bmcl.2006.05.077


[114]  Enantioselective synthesis of ferrocenyl nucleoside analogues with apoptosis-inducing activity, P. James, J. Neudorfl, M. Eissmann, P. Jesse, A. Prokop, H. G. Schmalz, Organic Letters20068, 2763-2766. 10.1021/ol060868f


[115]  Enantioselective synthesis of bicyclo 4.4.1 undecane-2,7-dione via samarium(II)-mediated fragmentation of a cyclopropane precursor, S. El Sheikh, N. Kausch, J. Lex, J. M. Neudorfl, H. G. Schmalz, Synlett 2006, 1527-1530.10.1055/s-2006-941599


[116]  A simple access to biologically important trans-stilbenes via Ru-catalyzed cross metathesis, J. Velder, S. Ritter, J. Lex, H. G. Schmalz,Synthesis-Stuttgart 2006, 273-278. 10.1055/s-2005-918506


[117]  Gold(I)-catalyzed reaction of 1-(1-alkynyl)-cyclopropyl ketones with nucleophiles: A modular entry to highly substituted furans, J. L. Zhang, H. G. Schmalz, Angewandte Chemie-International Edition 2006,45, 6704-6707. 10.1002/anie.200601252


[118]  Enantioselective organocatalysis in ionic liquids: Addition of aliphatic aldehydes and ketones to diethyl azodicarboxylate, P. Kotrusz, S. Alemayehu, T. Toma, H. G. Schmalz, A. Adler, European Journal of Organic Chemistry 2005, 4904-4911. 10.1002/ejoc.200500481


[119]  Total synthesis of (-)-colchicine via a Rh-triggered cycloaddition cascade, T. Graening, V. Bette, J. Neudorfl, J. Lex, H. G. Schmalz, Organic Letters 20057, 4317-4320. 10.1021/ol51316k


[120]  A Pauson-Khand approach to new carbocyclic nucleoside analogs, A. Lanver, H. G. Schmalz, European Journal of Organic Chemistry 2005, 1444-1458. 10.1002/ejoc.200400886


[121]  Microwave-assisted amination of a chloropurine derivative in the synthesis of acyclic nucleoside analogues, A. Lanver, H. G. Schmalz, Molecules 200510, 508-515. 10.3390/10020508


[122]  Application of chromium-arene complexes in the organic synthesis. Efficient synthesis of stilbene phytoalexins, K. E. Polunin, H. G. Schmalz,Russian Journal of Coordination Chemistry200430, 252-261. 10.1023/B:RUCO.0000022800.70211.7d


[123]  Michael additions of aldehydes and ketones to beta-nitrostyrenes in an ionic liquid, P. Kotrusz, S. Toma, H. G. Schmalz, A. Adler, European Journal of Organic Chemistry 2004, 1577-1583. 10.1002/ejoc.200300648


[124]  Iron-containing nucleoside analogues with pronounced apoptosis-inducing activity, D. Schlawe, A. Majdalani, J. Velcicky, E. Hessler, T. Wieder, A. Prokop, H. G. Schmalz, Angewandte Chemie-International Edition 2004,43, 1731-1734. 10.1002/anie.200353132


[125]  Pd-catalyzed cross-coupling of haloarenes and chloroarene-Cr(CO)(3) complexes with stabilized vinyl- and allylaluminium reagents, H. Schumann, J. Kaufmann, H. G. Schmalz, A. Bottcher, B. Gotov, Synlett 2003, 1783-1788.10.1055/s-2003-41492


[126]  Synthetic analogues of the antibiotic pestalone, F. Kaiser, H. G. Schmalz, Tetrahedron 200359, 7345-7355. 10.1016/s0040-4020(03)01136-0


[127]  Catalytic-enantioselective methoxycarbonylation of 1,3-dichloroarene-tricarbonyl-chromium(0) complexes: A desymmetrization approach to planar chirality, A. Bottcher, H. G. Schmalz, Synlett 2003, 1595-1598. 10.1055/s-2003-41417


[128]  An enantioselective approach to cytotoxic norcalamenenes via electron-transfer-driven benzylic umpolung of an arene tricarbonyl chromium complex, H. G. Schmalz, O. Kiehl, U. Korell, J. Lex, Synthesis-Stuttgart 2003, 1851-1855. 10.1055/s-2003-41030


[129]  Studies towards the total synthesis of mumbaistatin: synthesis of highly substituted benzophenone and anthraquinone building blocks, F. Kaiser, L. Schwink, J. Velder, H. G. Schmalz, Tetrahedron 200359, 3201-3217. 10.1016/s0040-4020(03)00427-7


[130]  Pd-catalyzed enantioselective allylic substitution: New strategic options for the total synthesis of natural products, T. Graening, H. G. Schmalz, Angewandte Chemie-International Edition 200342, 2580-2584. 10.1002/anie.200301644


[131]  Studies toward the total synthesis of mumbaistatin, a highly potent glucose-6-phosphate translocase inhibitor. Synthesis of a mumbaistatin analogue, F. Kaiser, L. Schwink, J. Velder, H. G. Schmalz, Journal of Organic Chemistry 2002,67, 9248-9256. 10.1021/jo026232t


[132]  An approach to serrulatane diterpenes via endo-selective conjugate nucleophilic addition to arene-Cr(CO)(3) complexes, F. Dehmel, J. Lex, H. G. Schmalz, Organic Letters 20024, 3915-3918. 10.1021/ol026827a


[133]  Identification of suitable ligands for a transition metal-catalyzed reaction: Screening of a modular ligand library in the enantioselective hydroboration of styrene, F. Blume, S. Zemolka, T. Fey, R. Kranich, H. G. Schmalz, Advanced Synthesis & Catalysis 2002344, 868-883. 10.1002/1615-4169(200209)344:8<868::Aid-adsc868>3.0.Co;2-m


[134]  eta(6)-Arene-tricarbonylchromium complexes in the syntheses of trans-resveratrol and pinostilbene, K. E. Polunin, I. A. Polunina, H. G. Schmalz, Mendeleev Communications 2002, 178-180. 10.1070/MC2002v012n05ABEH001616


[135]  Electron transfer driven transformations of transition metal pi-complexes: Samarium(II) iodide mediated coupling of fluoroarene-Cr(CO)(3) complexes with ketones, H. G. Schmalz, O. Kiehl, B. Gotov, Synlett 2002, 1253-1256. 10.1055/s-2002-32969


[136]  Chromium arene complexes in synthesis of trans-resveratrol, K. E. Polunin, H. G. Schmalz, L. A. Polunina, Russian Chemical Bulletin 200251, 1319-1324. 10.1023/a:1020921101384


[137]  Pd-catalyzed carbonylative cross-coupling reactions of chloroarene-Cr(CO)(3) complexes, B. Gotov, J. Kaufmann, H. Schumann, H. G. Schmalz, Synlett 2002, 1161-1163

[138]  Diallylaluminium-N,N-dimethylaminoethanolate, the first stable allyl-alane suitable for additions to aldehydes, ketones and imines, H. Schumann, J. Kaufmann, S. Dechert, H. G. Schmalz, Tetrahedron Letters 2002,43, 3507-3511. 10.1016/s0040-4039(02)00571-3


[139]  An efficient organometallic approach to new carbocyclic nucleoside analogues, J. Velcicky, J. Lex, H. G. Schmalz, Organic Letters 20024, 565-568. 10.1021/ol017181+


[140]  Synthesis and biological evaluation of new antimalarial isonitriles related to marine diterpenoids, O. Schwarz, R. Brun, J. W. Bats, H. G. Schmalz, Tetrahedron Letters 200243, 1009-1013. 10.1016/s0040-4039(01)02325-5


[141]  Pd-catalyzed cross-coupling of chloroarene-Cr(CO)(3) complexes with stabilized organoindium (III) reagents under remarkably mild conditions, B. Gotov, J. Kaufmann, H. Schumann, H. G. Schmalz, Synlett 2002, 361-363

[142]  Facile construction of the colchicine skeleton by a rhodium-catalyzed cyclization cycloaddition cascade, T. Graening, W. Friedrichsen, J. Lex, H. G. Schmalz, Angewandte Chemie-International Edition 2002,41, 1524-1526. 10.1002/1521-3773(20020503)41:9<1524::Aid-anie1524>3.0.Co;2-9


[143]  Benzylic endo-alkylation of phthalan-Cr(CO)(3) complexes via temporary silylation: An entry to trans-1,3-disubstituted dihydroisobenzofurans, S. Zemolka, J. Lex, H. G. Schmalz, Angewandte Chemie-International Edition 2002,41, 2525-+. 10.1002/1521-3773(20020715)41:14<2525::Aid-anie2525>3.0.Co;2-o


[144]  Gram-scale synthesis of suspension-polymerized styrene-divinylbenzene-based resins using an oscillatory baffled reactor, D. C. Sherrington, A. Lanver, H. G. Schmalz, B. Wilson, X. W. Ni, S. G. Yuan, Angewandte Chemie-International Edition 200241, 3656-3659. 10.1002/1521-3773(20021004)41:19<3656::Aid-anie3656>3.0.Co;2-7


[145]  Density functional investigation of reactive intermediates derived from alkyne-CO2(CO)(6) complexes, A. Pfletschinger, W. Koch, H. G. Schmalz, Chemistry-a European Journal 20017, 5325-5332. 10.1002/1521-3765(20011217)7:24<5325::Aid-chem5325>3.0.Co;2-s


[146]  Piceatannol, a hydroxylated analog of the chemopreventive agent resveratrol, is a potent inducer of apoptosis in the lymphoma cell line BJAB and in primary, leukemic lymphoblasts, T. Wieder, A. Prokop, B. Bagci, F. Essmann, D. Bernicke, K. Schulze-Osthoff, B. Dorken, H. G. Schmalz, P. T. Daniel, G. Henze, Leukemia 200115, 1735-1742. 10.1038/sj.leu.2402284


[147]  (CH2=CH)(2)Al(mu-OCH2CH2NMe2) (2): a vinylalane reagent suitable for conjugate additions to alpha,beta-unsaturated ketones, H. Schumann, J. Kaufmann, S. Dechert, H. G. Schmalz, J. Velder, Tetrahedron Letters 2001,42, 5405-5408. 10.1016/s0040-4039(01)01026-7


[148]  A catalytic-enantioselective entry to planar chiral pi-complexes: Enantioselective methoxycarbonylation of 1,2-dichlorobenzene-Cr(CO)(3), B. Gotov, H. G. Schmalz, Organic Letters 20013, 1753-1756. 10.1021/ol0159468


[149]  On the regioselectivity of nucleophilic additions to anisole-Cr(CO)(3) and related complexes: a density functional study, A. Pfletschinger, W. Koch, H. G. Schmalz, New Journal of Chemistry 200125, 446-450. 10.1039/b002898n


[150]  Kinetic investigation of the reduction of pinacolone by borane catalyzed by oxazaborolidines in THF. Hydride shift as rate determining step, H. Jockel, R. Schmidt, H. Jope, H. G. Schmalz, Journal of the Chemical Society-Perkin Transactions 2 2000, 69-76. 10.1039/a906935f


[151]  Structural and energetical characterization of the methylbutadiene-Fe(CO)(3) isomers and related reactive intermediates with quantum chemical methods, A. Pfletschinger, H. G. Schmalz, W. Koch, European Journal of Inorganic Chemistry 1999, 1869-1880

[152]  2-aminobenzimidazolium nitrate at 152 K, a triclinic crystal structure with pronounced local pseudo-symmetry, J. W. Bats, D. Gordes, H. G. Schmalz, Acta Crystallographica Section C-Crystal Structure Communications 1999,55, 1325-1328. 10.1107/s0108270199004710


[153]  Synthesis of an analog of the cytotoxic marine diterpene helioporin C exploiting arene-Cr(CO)(3) chemistry, D. Horstermann, H. G. Schmalz, G. Kociok-Kohn, Tetrahedron 199955, 6905-6916. 10.1016/s0040-4020(99)00346-4


[154]  Structural and energetical characterization of reactive intermediates derived from toluene-Cr(CO)(3), A. Pfletschinger, T. K. Dargel, J. W. Bats, H. G. Schmalz, W. Koch, Chemistry-a European Journal 19995, 537-545. 10.1002/(sici)1521-3765(19990201)5:2<537::Aid-chem537>3.0.Co;2-i


[155]  Memory of chirality in electron transfer mediated benzylic umpolung reactions of arene-Cr(CO)(3) complexes, H. G. Schmalz, C. B. de Koning, D. Bernicke, S. Siegel, A. Pfletschinger, Angewandte Chemie-International Edition 1999,38, 1620-1623. 10.1002/(sici)1521-3773(19990601)38:11<1620::Aid-anie1620>3.0.Co;2-1


[156]  Highly regioselective benzylic deprotonation of some (eta(6)-tetralin)- and (eta(6)-trans-octahydroanthracene)Cr(CO)(3) derivatives: Is the regioselectivity stereoelectronically controlled?", T. Volk, D. Bernicke, J. W. Bats, H. G. Schmalz, European Journal of Inorganic Chemistry 1998, 1883-1905

[157]  Electron transfer driven addition of ketimine derived radicals to arene-Cr(CO)(3) complexes, O. Hoffmann, H. G. Schmalz, Synlett 1998, 1426-1428

[158]  Electron transfer driven reactions of transition metal pi-complexes: Hydrogenation of styrene-Cr(CO)(3) derivatives by samarium(II)iodide in the presence of water, H. G. Schmalz, S. Siegel, D. Bernicke, Tetrahedron Letters 199839, 6683-6686. 10.1016/s0040-4039(98)01436-1


[159]  New developments in the Pauson-Khand reaction, O. Geis, H. G. Schmalz, Angewandte Chemie-International Edition 199837, 911-914. 10.1002/(sici)1521-3773(19980420)37:7<911::Aid-anie911>3.0.Co;2-o


[160]  On the oxazaborolidine-catalyzed borane reduction of 1-tetralone-Cr(CO)(3) complexes: The control of the reagent over a strong substrate, H. G. Schmalz, H. Jope, Tetrahedron199854, 3457-3464. 10.1016/s0040-4020(98)00078-7


[161]  Chiral arene-Cr(CO)(3) complexes in organic synthesis: A short enantioselective total synthesis of putative helioporin D, T. Geller, H. G. Schmalz, J. W. Bats, Tetrahedron Letters 199839, 1537-1540. 10.1016/s0040-4039(98)00021-5


[162]  Preparation of helioporin D from the seco-pseudopterosin aglycone: Revision of the stereostructure of helioporin D, T. Geller, J. Jakupovic, H. G. Schmalz, Tetrahedron Letters 199839, 1541-1544. 10.1016/s0040-4039(98)00020-3


[163]  Chiral eta(6)-arene-Cr(CO)(3) complexes as synthetic building blocks: A short enantioselective total synthesis of (+)-ptilocaulin, K. Schellhaas, H. G. Schmalz, J. W. Bats, Chemistry-a European Journal 19984, 57-66. 10.1002/(sici)1521-3765(199801)4:1<57::Aid-chem57>3.0.Co;2-h


[164]  Insertion of carbenoids into Cp-H bonds of ferrocenes: An enantioselective-catalytic entry to planar-chiral ferrocenes, S. Siegel, H. G. Schmalz, Angewandte Chemie-International Edition in English 199736, 2456-2458. 10.1002/anie.199724561


[165]  Kinetics of the borane reduction of pinacolone in THF catalyzed by two different oxazaboroles, R. Schmidt, H. Jockel, H. G. Schmalz, H. Jope, Journal of the Chemical Society-Perkin Transactions 2 1997, 2725-2731. 10.1039/a703700g


[166]  Enantioselective synthesis of the aglycones of pseudopterosin and seco-pseudopterosin via a common synthetic intermediate, A. Majdalani, H. G. Schmalz, Synlett 1997, 1303-&

[167]  On the deprotonation of eta(6)-1,3-dimethoxybenzene-Cr(CO)(3) derivatives: Influence of the reaction conditions on the regioselectivity, H. G. Schmalz, T. Volk, D. Bernicke, S. Huneck, Tetrahedron 199753, 9219-9232. 10.1016/s0040-4020(97)00620-0


[168]  Chiral eta(6)-arene-Cr(CO)(3) complexes in organic synthesis: A short and highly selective synthesis of the 18-nor-seco-pseudopterosin aglycone, A. Majdalani, H. G. Schmalz, Tetrahedron Letters 199738, 4545-4548. 10.1016/s0040-4039(97)00995-7


[169]  Enantioselective synthesis of new C-2-symmetric ferrocenylalkylamines via sonochemical amination of 1-ferrocenylalkyl acetates, M. Woltersdorf, R. Kranich, H. G. Schmalz, Tetrahedron 199753, 7219-7230. 10.1016/s0040-4020(97)00407-9


[170]  Synthesis of (E,E,E)-(1,2,3,4-C-13(4))-geranylgeraniol, K. Eis, H. G. Schmalz, Synthesis-Stuttgart 1997, 202-+

[171]  Controlling the course of nucleophilic additions to ortho-substituted (eta(6)-anisole)tricarbonyl-chromium complexes: Dienol ether formation versus tele-substitution, H. G. Schmalz, K. Schellhaas, Angewandte Chemie-International Edition in English 199635, 2146-2148. 10.1002/anie.199621461


[172]  Asymmetric induction in the nucleophile addition to eta(6)-arene-tricarbonyl-chromium(0) complexes, M. F. Semmelhack, H. G. Schmalz, Tetrahedron Letters 199637, 3089-3092. 10.1016/0040-4039(96)00572-2


[173]  Radical cyclization of eta(6)-arene-Cr(CO)(3) complexes: A regio- and stereoselective entry to functionalized pseudopterosin precursors, H. G. Schmalz, S. Siegel, A. Schwarz, Tetrahedron Letters 199637, 2947-2950. 10.1016/0040-4039(96)00486-8




[175]  CATALYTIC RING-CLOSING METATHESIS - A NEW, POWERFUL TECHNIQUE FOR CARBON-CARBON COUPLING IN ORGANIC-SYNTHESIS, H. G. Schmalz, Angewandte Chemie-International Edition in English 199534, 1833-1836. 10.1002/anie.199518331


[176]  Chemistry in Germany - off the defensive, C. Bolm, B. Frauendorf, A. Griesbeck, U. Kliem, A. Kretschmer, H. C. Militzer, G. Muller, H. Perry, H. J. Rosenkranz, H. G. Schmalz, W. Schnick, A. D. Schluter, R. Stadler, S. Waffenschmidt, Nachrichten Aus Chemie Technik Und Laboratorium 199543, 942-+




[180]  INTRAMOLECULAR ALKOXYPALLADATION, H. G. Schmalz, Nachrichten Aus Chemie Technik Und Laboratorium 199442, 1267-&

[181]  IRON-MEDIATED TOTAL SYNTHESIS OF IKARUGAMYCIN, H. G. Schmalz, Nachrichten Aus Chemie Technik Und Laboratorium 199442, 1016-&



[183]  ZIRCONIUM-CATALYZED CARBOMAGNESATION, H. G. Schmalz, Nachrichten Aus Chemie Technik Und Laboratorium 199442, 724-729

[184]  AN APPROACH TO CHIRAL ETA(4)-BUTADIENE-FE(CO)(3) COMPLEXES VIA DIASTEREOSELECTIVE COMPLEXATION OF NONRACEMIC 2-ALKOXY-4-VINYL-2,5-DIHYDROFURAN DERIVATIVES, H. G. Schmalz, E. Hessler, J. W. Bats, G. Durner, Tetrahedron Letters 199435, 4543-4546. 10.1016/s0040-4039(00)60723-2


[185]  CHIRAL ETA-4-BUTADIENE-FE(CO)3 COMPLEXES FOR ORGANIC-SYNTHESIS - REACTIONS OF (ETA(4)-2-ALKOXY-4-VINYL-2,5-DIHYDROFURAN)-FE(CO)(3) DERIVATIVES, E. Hessler, H. G. Schmalz, G. Durner, Tetrahedron Letters 199435, 4547-4550. 10.1016/s0040-4039(00)60724-4


[186]  PD-CATALYZED SYNTHESIS OF VITAMIN-D ACTIVE COMPOUNDS, H. G. Schmalz, Nachrichten Aus Chemie Technik Und Laboratorium 199442, 394-&

[187]  ENANTIOSELECTIVE HECK REACTIONS, H. G. Schmalz, Nachrichten Aus Chemie Technik Und Laboratorium 199442, 270-&

[188]  CHROMIUM CARBENE COMPLEXES IN ORGANIC-SYNTHESIS - RECENT DEVELOPMENTS AND PERSPECTIVES, H. G. Schmalz, Angewandte Chemie-International Edition in English 199433, 303-305. 10.1002/anie.199403031




[190]  TOTAL SYNTHESIS OF (1S,4S)-7,8-DIHYDROXYCALAMENENE VIA BENZYLIC ALKYLATION OF ETA(6)-ARENE-CR(CO)3 COMPLEXES, H. G. Schmalz, J. Hollander, M. Arnold, G. Durner, Tetrahedron Letters 199334, 6259-6262. 10.1016/s0040-4039(00)73725-7


[191]  TOTAL SYNTHESIS OF THE PSEUDOGUAIANOLIDE (+)-CONFERTIN, G. Quinkert, H. G. Schmalz, E. Walzer, S. Gross, T. Kowalczykprzewloka, C. Schierloh, G. Durner, J. W. Bats, H. Kessler, Liebigs Annalen Der Chemie 1988, 283-315


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