Stephane Caron

Synthesis of 1-Substituted 3-Aryl-5-aryl(hetaryl)-2-pyrazolines and Study of Their Antitumor Activity

Archiv der Pharmazie, 2011

Three series of novel 1,3,5-trisubstituted 2-pyrazoline derivatives containing thiophene and benz... more Three series of novel 1,3,5-trisubstituted 2-pyrazoline derivatives containing thiophene and benzodioxol moieties as potential antitumor agents were synthesized. The in vitro antitumor activity of the obtained compounds was determined at the National Cancer Institute (NCI). The 5-(benzo[d][1,3]dioxol-5-yl)-3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide (9a) is the most prominent of the compounds due to its remarkable activity toward leukemia (RPMI-8226), renal cancer (UO-31) and prostate cancer (DU-145) cell lines with GI 50 values of 1.88, 1.91 and 1.94 mM, respectively.

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Total Synthesis of Zaragozic Acid A/Squalestatin S1

Angewandte Chemie International Edition in English, 1994

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Fundamentals of Early Clinical Drug Development: From Synthesis Design to Formulation. Edited by A. F. Abdel-Magid and Stéphane Caron

ChemMedChem, 2007

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Processes and intermediates for preparing substituted indazole derivatives

Preparation of N1-Phenylacetamidine 4-Bromobenzoate Using 2,2,2-Trichloroethyl Acetimidate Hydrochloride

Organic Syntheses, 2013

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Preparation of N1-Phenylacetamidine 4-Bromobenzoate Using 2,2,2-Trichloroethyl Acetimidate Hydrochloride

Organic Syntheses, 2013

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Synthesis of Aromatic Diterpenes Synthesis of 12-Hydroxy-abieta-8,11,13-trien-3,7-dione

Synthetic Communications, 1991

ABSTRACT Model studies involving cationic cyclisation of suitable dienes have provided a synthesi... more

New ligands for nickel catalysis from diverse pharmaceutical heterocycle libraries

Nature Chemistry, 2016

Ligands are essential for controlling the reactivity and selectivity of transition metal-catalyze... more Ligands are essential for controlling the reactivity and selectivity of transition metal-catalyzed reactions. Access to large phosphine ligand libraries has become an essential tool for the application of metal-catalyzed reactions industrially, but these existing libraries are not well suited to new catalytic methods based on non-precious metals (i.e., Ni, Cu, Fe). The development of the requisite nitrogen-and oxygen-based ligand libraries lags far behind phosphines and the development of new libraries is anticipated to be time consuming. Here we show that this process can be dramatically accelerated by mining a typical pharmaceutical compound library that is rich in heterocycles for new ligands. Using this approach, we were able to screen a structurally diverse set of compounds with minimal synthetic effort and identify several new ligand classes for nickelcatalyzed cross-electrophile coupling. These new ligands gave improved yields for challenging cross-couplings of pharmaceutically relevant substrates compared to previously published ligands.

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Methods of preparing 4-cyano-4-(substituted indazole)cyclohexane-carboxylic acids useful as PDE4 inhibitors

Substituted Aryl Boronic Acids, Their Preparation and Their Precursors

Substituted Pyridines via Boronic Acid Coupling

Processes for preparing substituted aryl boronic acids

Methods for preparing N-arylated oxazolidinones via a copper catalyzed cross coupling reaction

ChemInform Abstract: Synthesis of the ϰ-Agonist CJ-15,161 via a Palladium-Catalyzed Cross-Coupling Reaction

Cheminform, 2010

Processes for preparing substituted chromanol derivatives

Process for preparing 2-phenyl-3-aminopyridine, substituted phenyl derivatives thereof, and salts thereof

Preparation of Tertiary Benzylic Nitriles from Aryl Fluorides

J Am Chem Soc, 2000

... H.; Smejkal, RM; Payne, CS; Padilla, FN; Doctor, BP; Gordon, RK; Chiang, PK J. Med. Chem.1989... more

Process Research and Development of an NK-1 Receptor Antagonist. Enantioselective Trifluoromethyl Addition to a Ketone in the Preparation of a Chiral Isochroman

Organic Process Research Development, 2007

CJ-17,493 (4) is a chiral NK-1 receptor antagonist. It was first prepared through a diastereosele... more

2,3-SUBSTITUTED Indole Compounds as COX-2 Inhibitors

Benzyl(idene)-lactam derivatives

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