Merck Sharp + Dohme Corp.

Schering Corporation

Kelvin Yong

Xiaoyong Fu

Jianguo Yin

Ilia A Zavialov

Guy R Humphrey

Tiruvettipuram K Thiruvengadam

Hongmei Li

Timothy L McAllister

Cheng Yi Chen

Michael J Zacuto

Shuyi Zhang

Bangping Xiang

Michael R Reeder

Matthew Thomas Tudge

Jongrock Kong

Timothy D Cutarelli

Sarah Dolman

Thiruvettipuram K Thiruvengadam

The present invention relates to macrolactam compounds, intermediates useful in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing and modifying macrolactams. One use of the compounds and methods described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. An example of an HCV inhibitory compound that can be synthesized using the procedures described herein is Compound A and derivative thereof.

Process and intermediates for preparing macrolactams

This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein Ris selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and Ris selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, Xis Cl, Br, or I; Xis selected from Cl and Br; and PdLis a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.

Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate

This application discloses a novel process to synthesize 2-(Quinolin-5yo)-4,5-Disubstituted-Azole derivatives, which may be used, for example, as PDE IV inhibitor compounds in pharmaceutical preparations.

Process and intermediates for the synthesis of 2-(quinolin-5-yl)-4,5 disubstituted-azole derivatives

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Lyndhurst, NJ, United States of America

Kelvin Yong