Schering Corporation

Merck Sharp + Dohme Corp.

Opko Health, Inc.

Tesaro, Inc.

Merck Sharp & Dohme LLC

Frank Xing Chen

Mingsheng Huang

Tao Wang

Marc Poirier

Daw-long Kwok

Ngiap Kie Lim

Jian Cui

Vijay Sabesan

Xiaojing Yang

Ji Xie

George G Wu

Tiruvettipuram K Thiruvengadam

Anantha R Sudhakar

Yee-Shing Wong

Jing Liao

Hoa N Nguyen

Nobuyoshi Yasuda

Joseph E Lynch

Shen-Chun Kuo

Yong-Li Zhong

Jianguo Yin

Ilia A Zavialov

Nanfei Zou

Carmela Molinaro

Hong-Chang Lee

Daw-long Albert Kwok

W Peter Wuelfing

Teresa Andreani

Charles F Bernard

Paitoon Rashatasakhon

Victoria M Sprague

Xiaoyong Fu

George S K Wong

Feng Liang

Peter C Nirchio

Gerald Werne

Jennifer Ann Vance

Alistair Stewart

Anthony Joseph Toto

Michael Casey

Denise C Grogan

Nolan C Erickson

Liansheng Zeng

Louis Peter Castellanos

Yuyin Chen

Daw-Iong Albert Kwok

Maria M Tamarez

Vijay Sabesen

Illia Zavialov

Ilia Zavialov

Zou Nanfei

Daw-Long Kwok

Jeffrey M Eckert

Kartik M Keertikar

George S Wong

Jeffrey Manning Eckert

Robert Kevin Orr

Ingrid Mergelsberg

David Jieh-Shyh Tsai

Agnes S Kim-Meade

Fucheng Zhang

Juergen Weber

Robert Parry Williams

Donald Hou

Ramani R Raghavan

George Wu

Disclosed herein are methods and processes of preparing niraparib and pharmaceutically acceptable salts thereof, and intermediates and their salts useful for the synthesis of niraparib.

Methods of manufacturing of niraparib

The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine.

Intermediates for preparing CGRP receptor antagonists

Process for making CGRP receptor antagonists

This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.

Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds

The disclosure encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, having less steps and improved yields as compared to previous synthetic methods for making these compounds, which are CGRP receptor antagonists, useful for the treatment of migraine. Conditions for an amide bond formation between an acid and amine include for example reacting the compounds of Formulae B (after salt break) and C with an amide coupling reagent and optionally an additive and an acid and/or a base in a non-reactive solvent.

This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following: 

Exo- and diastereo-selective synthesis of himbacine analogs

Exo- and diastereo- selective synthesis of himbacine analogs

The present invention provides for a process for preparing racemic methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate, its corresponding salt: (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-D-tartaric acid ('D-DTTA') salt or a (1S,2R,5R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-L-tartaric acid salt ('L-DTTA') in a high enantiomeric excess. This invention also provides for a process for preparing a (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate dibenzoyl-D-tartaric acid (&#x201c;D-DBTA&#x201d;) salt or a (1S,2R,5R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate L-tartaric acid (&#x201c;L-DBTA&#x201d;) salt in a high enantiomeric excess. Further, this invention provides a process for preparing intermediates II, IIB, III, IV, IV salt, V, VI, and VII.

Process for the preparation of 6,6-dimethyl-3-azabicyclo-[3.3.0]-hexane compounds and enantiomeric salts thereof

Disclosed is a process for the synthesis of compounds of Formula I by sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1, wherein Ris a linear, branched, or cyclic alkyloxy functional group of the structure (&#x2014;R&#x2014;OH), Ris a linear, branched or cyclic alkyl group, Ris a linear, branched or cyclic alkyl group, and Ris an alkylene-heterocycle, said process comprising forming intermediate compound of Formula E1 by reacting, in a refluxing reaction solvent selected from alcohols having 5 or less carbon atoms and mixtures of two or more thereof, a methanol solution of a salt of a 4-alkyl-3-amino-pyrazole compound of Formula C1, with a diamidization reagent selected from dimethylmalonate, monomethylmalonyl-chloride, and malonyl dichloride in the presence of a Lewis base having sufficient proton affinity to abstract a proton from the 1-position nitrogen on the pyrazole ring.

Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates

Exo- and diastereo-selective syntheses of himbacine analogs

The present invention provides a method of resolving piperdin-yl-alkylene-alcohols, in high yield at high enantiomeric purity, for example 2-piperidin-2-yl-ethanol.

Process for resolving chiral piperidine alcohol and process for synthesis of pyrazolo[1,5-a] pyrimidine derivatives using same

The present invention provides for a process for preparing racemic methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate, its corresponding salt: (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-D-tartaric acid ('D-DTTA') salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-L-tartaric acid salt ('L-DTTA') in a high enantiomeric excess. This invention also provides for a process for preparing a (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate dibenzoyl-D-tartaric acid (&#x201c;D-DBTA&#x201d;) salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate L-tartaric acid (&#x201c;L-DBTA&#x201d;) salt in a high enantiomeric excess. Further, this invention provides a process for preparing intermediates II, IIB, III, IV, IV salt, V, VI, and VII.

Process for the preparation of 6,6-dimethyl-3-azabicyclo-[3.1.0]-hexane compounds and enantiomeric salts thereof

Exo- and diastereo- selective syntheses of himbacine analogs

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Plainsboro, NJ, United States of America

Frank Xing Chen