Bristol-myers Squibb Compnay

James H Simpson

Yi Xiao

Boguslaw Mudryk

Martin D Eastgate

Jonathan Clive Tripp

Richard J Fox

Ke Chen

Michael S Bultman

Dayne Dustan Fanfair

Thomas E La Cruz

Christina Ann Risatti

Maxime C Soumeillant

David R Kronenthal

Rajendra P Deshpande

Ramesh N Patel

Mark E Salvati

Bang-Chi Chen

Ronald L Hanson

William John Winter

John J Venit

Jerome L Moniot

Toomas Mitt

Paul Alan Jass

Shawn K Pack

Animesh Goswami

John L Dillon, Jr

Sushil K Srivastava

Keith Ramig

Edward J Delaney

David B Brzozowski

Shankar Swaminathan

Mark D Schwinden

William Aloysius Nugent

Saibaba Racha

Wen-sen Li

Theodor W Denzel

Keming Zhu

Chien-Kuang Chen

Linda Nga Hoong Chu

Michael J Totleben

Weixuan He

A method for making the compound is set forth utilizing the starting material 

Methods for the preparation of HIV attachment inhibitor piperazine prodrug compound

A method for making the compound is set forth utilizing the starting material wherein R&#x2550;&#x2014;H, alkyl, aryl, &#x2014;SOR, &#x2014;C(O)OR, and &#x2014;C(O)NR; where R&#x2550;&#x2014;H, C-Calkyl, -aryl, and &#x2014;CHAryl.

Methods for the Preparation of HIV attachment inhibitor piperazine prodrug compound

A process for the preparation of the compound of Formula I is set forth utilizing the starting compound 1 and the acid chloride compound 

A process for preparing Z-5-carboxymethylene-1,3-dioxolan-4-ones is provided which includes the steps of reacting a bis-ketal or bis-acetal of tartaric acid with a potassium containing base to form the carboxymethylene-1,3-dioxolan-4-one. A process for preparing HIV integrase inhibitors employing the carboxymethylene-1,3-dioxolan-4-one inhibitor is also provided.

Process for the preparation of Z-5-carboxymethylene-1,3-dioxolan-4-ones

Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

Method for the preparation of fused heterocyclic succinimide compounds and analogs thereof

Mercaptoalkanoylamino lactam acids are recrystallized by treatment with an agent that minimizes the formation of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite.

Recrystallization processes

Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the amount of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite. Such agents are also employed in the recrystallization and reprocessing of the mercaptoalkanoylamino lactam acids.

Deprotection and recrystallization processes

N-protected-L-homocysteine disulfide of the formula ##STR1## or an activated form thereof is reacted with (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester to give the disulfide intermediate of the formula ##STR2## Cleavage of the disulfide bond followed by acid catalyzed cyclization produces the N-protected lactam of formula III which is useful for preparing the pharmaceutically active compound omapatrilat.

Preparation of

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Hillsborough, NJ, United States of America

James H Simpson