Schering Corporation

Opko Health, Inc.

Merck Sharp + Dohme Corp.

Ji Xie

Frank Xing Chen

George G Wu

Marc Poirier

Jian Cui

Anantha R Sudhakar

Tiruvettipuram K Thiruvengadam

Xiaojing Yang

Tao Wang

Jing Liao

Hoa N Nguyen

Mingsheng Huang

Ngiap Kie Lim

Vijay Sabesan

Ilia A Zavialov

Daw-long Albert Kwok

Victoria M Sprague

Xiaoyong Fu

Robert Kevin Orr

Ingrid Mergelsberg

Fucheng Zhang

Gerald Werne

Yuyin Chen

Liansheng Zeng

Louis Peter Castellanos

Shen-Chun Kuo

Kartik M Keertikar

Hong-Chang Lee

Ramani R Raghavan

Daw-Iong Albert Kwok

Maria M Tamarez

Paitoon Rashatasakhon

Vijay Sabesen

Illia Zavialov

Daw-Long Kwok

Ilia Zavialov

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

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

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

Exo- and diastereo- selective syntheses of himbacine analogs

The present application relates to a process for preparing a compound of formula I:  

Oxidation process for the preparation of N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-{N-[(tert-butylamino)carbonyl]-3-methyl-L-valyl}-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide and related compounds

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Edison, NJ, United States of America

Ji Xie