Schering Corporation

Merck Sharp + Dohme Corp.

Scinopharm (changshu) Pharmaceuticals, Ltd.

Schering-plough Corporation

Scinopharm Pharmaceuticals, Ltd.

Shen-Chun Kuo

Loc Thanh Tran

Pengyi Zhang

Donald Hou

David Jieh-Shyh Tsai

Frank Xing Chen

Andrew D Jones

Janet L Mas

George G Wu

Hongbiao Liao

Yonggang Chen

Guo-dong Chu

Yi-Jing Chen

Stanislaw Pikul

F George Njoroge

Frank W Bennett

Nobuyoshi Yasuda

Ashok Arasappan

Stephane L Bogen

David J Blythin

John Fitzgerald Traverse

William W Leong

Kartik M Keertikar

Peter Emmanuel Maligres

Marc Poirier

Edward Cleator

Jianguo Yin

Kevin Michael Belyk

Nanfei Zou

Jeffrey Manning Eckert

William Kreutner

Scott Trzaska

Hong-Chang Lee

Ji Xie

Agnes S Kim-Meade

Ramani R Raghavan

Bangping Xiang

Jianshe Kong

Kenneth Stanley Matthews

Charles F Bernard

Jennifer Albaneze-Walker

Lijun Wang

Steven P Miller

William M Leong

Zheng-Yun Zhan

Randi M Smith

Donald Chen-tung Hou

Gabriel C Kuklis

Amadeo Ferreira

Patrice Demonchaux

Azzeddine Lekhal

Thomas J Hunter

Scott T Trzaska

Kevin M Belyk

Youggang Chen

Jeffrey M Eckert

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, utilizing a highly effective spiroacid synthesis.

Process for making CGRP receptor antagonists

The present invention provides novel processes for the preparation of N-substituted benzamides having the formula VIc: In some embodiments, the invention provides a process for preparation of roflumilast and other pharmaceutically active species. Novel compounds, including intermediates for the synthesis of roflumilast, are also provided.

Process for preparation of roflumilast

The present invention provides novel processes for the preparation of N-substituted benzamides having the formula (VIc). In some embodiments, the invention provides a process for preparation of roflumilast and other pharmaceutically active species. Novel compounds, including intermediates for the synthesis of roflumilast, are also provided. 

Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed. 

Enantio- and stereo specific synthesis of &#x3b2;-amino-&#x3b1;-hydroxy amides

A process for preparing 7-[2-[4-(6-fluoro-3-methyl-1,2-benzisoxazol-5-yl)-1-piperazinyl]ethyl]-2-(1-propynyl)-7H-pyrazolo-[4,3-e]-[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, intermediates useful in that process, and processes for preparing said intermediates are disclosed.

Process for preparing a 2-alkynyl substituted 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine

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

The present invention discloses a novel process to prepare ketone amides, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 1-(2,4-dimethylpyrimidine-5-carbonyl)-4-piperidone, 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4-piperidone and related compounds. A salient feature of the invention is the use of a three-phase reaction medium with an organic phase and a buffer salt slurry.

Preparation of ketone amides

This invention relates to a novel process for the synthesis of Temozolomide, an antitumor compound, and analogs, and to intermediates useful in this novel process.

Synthesis of temozolomide and analogs

A process for preparing substituted 5-amino-pyrazolo[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidine compounds having an aminoalkyl substituent at the 7-position is disclosed, wherein the pyrimidine ring is cyclized using a cyanating agent.

Process for preparing substituted 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines

A process for preparing substituted 5-amino-pyrazolo[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidine compounds having an aminoalkyl substituent at the 7-position is disclosed.

Process for preparing substituted 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidines

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Union, NJ, United States of America

Shen-Chun Kuo