Bristol-myers Squibb Compnay

Xuebao Wang

Richard P Polniaszek

John K Thottathil

Yadagiri R Pendri

Eduardo J Martinez

Jeffrey S DePue

Kumar G Gadamasetti

Chennagiri R Pandit

Robert Zahler

Ping Chen

Joel C Barrish

Steven H Spergel

Peter T Cheng

Apurba Bhattacharya

John Anthony Grosso

Edward J Delaney

Ambarish K Singh

Theodor W Denzel

Chien-Kuang Chen

Wangying Yang

Melissa Chau

Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension.

Methods for the preparation of biphenyl isoxazole sulfonamides

An improved process is provided for synthesis of a halomethyl benzoic acid chloromethyl ester, a key intermediate for use in production of azole antifungal compounds and other pharmaceutical products.

Process for azole antifungal intermediate

Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates therof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension, congestive heart failure and male erectile dysfunction.

A process for preparing optically active (S)-(-) and (R)-(+)-deoxyspergualin and salts thereof of the formula I ##STR1## by reacting a compound of formula II ##STR2## with a compound of formula III ##STR3## in the presence of a condensing/dehydrating agent and an organic or inorganic base in an organic solvent to form a compound of formula IV ##STR4## which can then be converted to the desired final product of formula I via deprotection and hydrogenolysis. The invention also comprises the compounds of the formula II, IV and VII ##STR5##

Preparation of optically active (S)-(-) and (R)-(+)-deoxyspergualin and

The present invention relates to a novel method useful for the conversion of amino acids to halomethylketones, which are then converted to amino acid epoxides. Such epoxides are important intermediates for the synthesis of inhibitors of renin and HIV protease, which are particularly useful in the treatment and/or prevention of HIV infection (AIDS).

Process for preparing N-protected amino acid .alpha.-halomethyl ketones

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East Brunswick, NJ, United States of America

Xuebao Wang