Bristol-myers Squibb Compnay

Rajendra P Deshpande

David R Kronenthal

Jun Li

James H Simpson

Jeffrey A Robl

James J Li

Bang-Chi Chen

Chenkou Wei

Jerome L Moniot

Lawrence J Kennedy

Joydeep Kant

Michael A Galella

Xinhua Qian

Haixia Wang

Susan D Boettger

Jing Liang

Neal G Anderson

Edward J Gublo

Ulhas P Dhokte

Theodor W Denzel

Jie Jack Li

Laxma Reddy Kolla

Reginald O Cann

Frank S Gibson

Karen L TenHuisen

Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula I: or stereoisomers or pharmaceutically acceptable salts thereof, wherein G, Q, X, Y, R, R, and Rare defined herein.

Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors

A process is provided for preparing 4-alkyl- or 4-aryl-oxycarbonyl paclitaxel analogs which includes the steps of converting paclitaxel into a C-7 acylprotected paclitaxel employing an electrophilic protecting group, such as benzoyloxycarbonyl, and converting the C-7 protected analog into the 4-alkyloxycarbonyl or 4-aryloxycarbonyl paclitaxel analog. Novel intermediates produced in the process are also provided.

Process for preparing 4-alkyl- or 4-aryl-oxycarbonyl paclitaxel analogs and novel intermediates

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 phosphate reducing agents, zinc metal powder, and sodium hydrosulfite.

Deprotection 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

Disclosed is a process for preparing N-substituted heterocyclic derivatives and its salts using phase transfer catalysis.

Method for preparing N-substituted heterocyclic derivatives using a

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Hillsborough, NJ, United States of America

Rajendra P Deshpande