Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Millennium Pharmaceuticals Limited

Portola Pharmaceuticals, Inc.

Banyu Pharmaceutical Co. Ltd

Zhiguo Jake Song

Feng Xu

Anjali Pandey

Jeffrey C Moore

David M Tschaen

Laura Marie Artino

Guy R Humphrey

David J Mathre

John Y L Chung

Lushi Tan

Tao Wang

Guo-Jie Ho

Michael J Zacuto

Tao Pei

Yonggang Chen

John S Wai

Peter D Williams

Paul N Devine

Shankar Venkatraman

Wayne J Thompson

Richard John Varsolona

Vinay M Girijavallabhan

Richard D Tillyer

Dai-Shi Su

David M Tellers

Erika M Milczek

Mark W Embrey

Peter Emmanuel Maligres

Yong-Li Zhong

Edward Cleator

Jeonghan Park

Michael J Williams

Thorsten E Fisher

David L Hughes

Paul Sohar

Richard F Shuman

Andrew William Gibson

Mangzu Zhao

Qinghao Chen

Yang Cao

Khateeta M Emerson

Mark McLaughlin

Feng Peng

Mathew Thomas Maust

Amude Kassim

Cheng-yi Chen

Emilia P T Leitao

Jose Rato

Jing Li

Stephen Philip Keen

Ji Qi

Yaling Wang

Eiichi Mano

Jingjun Yin

Richard Desmond

David R Lieberman

J Michael Williams

David C Dubost

Michael Shevlin

Neil A Strotman

Richard C A Isaacs

Matthew L Maddess

Dietrich P Steinhuebel

Richard G Ball

Rebecca T Ruck

Eric J Choi

Hongming Li

Kimberly A Savary

David A Mathre

Jongrock Kong

Sarah L Trice

Neil Campbell

Emilia P Leitao

Alejandro Dieguez Vazquez

Mark Mclaughlin

Kevin M Belyk

Matthew Maddess

A process for preparing a compound of structural Formula Ia:   

Process for preparing chiral dipeptidyl peptidase-IV inhibitors

The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.

Methods and intermediates for preparing macrolactams

A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of, reductive amination of: 

The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams from the intermediates. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.

Process and intermediates for preparing macrolactams

Described herein are novel methods of preparing a compound of Formula II or a pharmaceutically acceptable salt thereof. In some embodiments, the method is for preparing betrixaban or a pharmaceutically acceptable salt thereof. Also described are compositions comprising substantially pure betrixaban free base or salt thereof. 

Methods of synthesizing factor Xa inhibitors

The present invention relates to synthetic processes useful in the preparation of macrocyclic compounds of Formula (I) that are useful as inhibitors of the hepatitis C virus NS3 protease and have application in the treatment of conditions caused by the hepatitis C virus. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation. 

Processes for preparing protease inhibitors of hepatitis C virus

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X, X, Y, R, R, Rand Rare defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.

HIV integrase inhibitors

A novel process is provided for the preparation of ribofuranose sugar derivatives which are useful in the synthesis of branched-chain ribonucleoside inhibitors of HCV polymerase for the treatment of HCV infection. Also provided are useful intermediates obtained from the instant process.

Process to ribofuranose sugar derivatives as intermediates to branched-chain nucleosides

The present invention relates to a periodic acid oxidation which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula I having a carboxylic acid.

Oxidation process using periodic acid

The present invention relates to an oxidation which converts a primary or secondary alcohol of Formula II: ##STR1## to an acid or ketone of Formula I: ##STR2## with periodic acid and a catalytic amount of a chromium reagent.

The present invention relates to a TEMPO-catalyzed oxidation of primary alcohols, RCH.sub.2 OH to corresponding carboxylic acids, RCOOH in the presence of catalytic in the presence of catalytic amount of NaClO and stoichiometric amount of NaClO.sub.2 as an oxidant. ##STR1##

Oxidaton of primary alcohols to carboxylic acids with a TEMPO catalyst

This invention relates to a cyclization process useful in the preparation of a key intermediate in the preparation of an endothelin antagonist of the general formula shown below: ##STR1##

Phosphate-mediated cyclization

The present invention relates to an oxidation using sodium chlorite in the presence of a catalytic amount of TEMPO and sodium hypochlorite which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula I having a carboxylic acid ##STR1##

Oxidation process using tempo

Imidazolmethyloxy-substituted tricyclo-macrolide immunosuppressants are prepared by reacting a tricyclo-macrolide with an imidazolmethyl trichloroacetimidate in the presence of an acid. The invention further provides a crystalline salt of imidazolmethyloxy-substituted tricyclo-macrolide, as well as novel compounds useful in the process of the present invention.

Process for the preparation of imidazolyl macrolide immunosuppressants

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Edison, NJ, United States of America

Zhiguo Jake Song