Merck Sharp + Dohme Corp.

California Institute of Technology

Merck Sharpe & Dohme Corp.

Cardiome International Ag

Cheol Keun Chung

Guy R Humphrey

John Limanto

Mark E Scott

Kevin Michael Belyk

Paul Gerard Bulger

Zhijian Liu

Robert H Grubbs

Jacob M Janey

Younong Yu

Gregory Hughes

Peter Emmanuel Maligres

Artis Klapars

Hallena Strotman

Gregory L Beutner

Jingjun Yin

Matthew D Truppo

Eric Ashley

Mark McLaughlin

Yingju Xu

Timothy James Wright

Kevin Kuhn

Brendan Grau

Jean-Baptiste Bourg

Hallena R Strotman

Eric R Ashley

A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.

Regioselective N-2 arylation of indazoles

Disclosed herein is a novel process for preparing substituted quinazoline compounds of formula (I) using a hydrogen bonding catalyst. 

Processes for making substituted quinazoline compounds using hydrogen bonding catalysts

An efficient process is disclosed for producing the compound of formula I, which is the CETP inhibitor anacetrapib, which raises HDL-cholesterol and reduces LDL-cholesterol in human patients and may be effective for treating or reducing the risk of developing atherosclerosis: 

Process for synthesizing a CETP inhibitor

The present invention relates to a process for preparing aminocyclohexyl ether compounds of Formula I: or the pharmaceutically acceptable salts and esters thereof. In particular, the instant invention is directed towards a process for preparing (1R,2R)-2-[(3R)-Hydroxypyrrolidinyl]-1-(3,4-dimethoxyphenethoxy)-cyclohexane as well as various intermediates. 

Process for preparing aminocyclohexyl ether compounds

This invention relates generally to olefin metathesis, more particularly, to tri- or tetra-substituted imidazolinium salts which are precursors to N-heterocyclic carbene (NHC) ligands with tri- or tetra-substituted imidazolinium rings, organometallic ruthenium complexes comprising gem di-substituted imidazolinium NHC ligands, organometallic ruthenium complexes comprising tri- or tetra-substituted imidazolinium NHC ligands, and to olefin metathesis methods using them. The catalysts and methods of the invention have utility in the fields of catalysis, organic synthesis, and industrial chemistry.

Ruthenium olefin metathesis catalysts bearing N-heterocyclic carbene ligands with substituted backbone

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Westfield, NJ, United States of America

Cheol Keun Chung