Pfizer Corporation

John Wing Wong

Michael P Burns

Robert Wayne Dugger

Robert James Chambers

Yong Tao

Ming Kang

Justin K Weaver

James J Cawley

Nobuji Yoshikawa

Susan J Truesdell

Brook K Morse

Susan J I Truesdell

Akemi Sugiura

Yutaka Sugie

The present invention is directed to a regio-and stereoselective bioconversion of selected aliphatic dinitriles into corresponding cyanocarboxylic acids. More particularly, the present invention provides methods for the conversion of 2-isobutyl-succinonitrile into (S)-3 cyano-5-methylhexanoic acid, which is a useful intermediate in the synthesis of (S)-3(aminomethyl)-5-methylhexanoic acid (pregabalin). Pregabalin can be used for treating certain cerebral diseases, for example, in the treatment and prevention of seizure disorders, pain, and psychotic disorders.

Stereoselective bioconversion of aliphatic dinitriles into cyano carboxylic acids

The present invention is directed to a regio- and stereoselective bioconversion of selected aliphatic dinitriles into corresponding cyanocarboxylic acids. More particularly, the present invention provides methods for the conversion of 2-isobutyl-succinonitrile into (S)-3 cyano-5-methylhexanoic acid, which is a useful intermediate in the synthesis of (S)-3(aminomethyl)-5-methylhexanoic acid (pregabalin). Pregabalin can be used for treating certain cerebral diseases, for example, in the treatment and prevention of seizure disorders, pain, and psychotic disorders.

The present invention provides processes useful in the preparation of certain &#x3b2;-adrenergic receptor agonists of the structural formulathe pharmaceutically acceptable salts thereof, and the hydrates of said pharmaceutically acceptable salts, wherein HET is as described herein. The invention further provides intermediates useful in the preparation of such agonists, and processes useful in the production of such intermediates.

Processes and intermediates useful in preparing &#x3b2;3-adrenergic receptor agonists

The present invention relates to processes for the microbial oxidation of bicyclic heteroaromatic compounds which comprise contacting these compounds with a microorganism, or a suitable mutant thereof, and incubating the resulting mixture under conditions sufficient to yield an amount of their respective carboxylic acids. The present processes optionally further comprise the isolation and purification of the product carboxylic acids.

Microbial conversion of bicyclic heteroaromatic compounds

Processes and intermediates useful in preparing &bgr;3-adrenergic receptor agonists

Microbial process for preparation of optically active 3-hydroxypyrrolidine derivatives

Stereoselective microbial reduction of a racemic tetralone

The present invention relates to microbial processes for carrying out the asymmetric reduction of a ketone to an alcohol, which comprises: contacting the ketone with a microorganism, or an enzyme reduction system capable of accomplishing the subject reduction comprising an enzyme derived from said microorganism and a co-factor for said enzyme, and incubating the resulting mixture under conditions sufficient to yield more of the desired (R)-enantiomer of the corresponding alcohol than the undesired (S)-enantiomer. The chiral (R)-enantiomer can be used in the synthesis of certain &bgr;-adrenergic receptor agonists.

Microbial asymmetric reduction of 2-chloro-1-&lsqb;-6-(2,5-dimethyl-pyrrol-1-yl)-pyridin-3-yl&rsqb;-ethanone

The present invention relates to processes for the microbial oxidation of 2-methylquinoxaline to 2-quinoxalinecarboxylic acid which comprise contacting 2-methylquinoxaline with a microorganism, or a suitable mutant thereof, and incubating the resulting mixture under conditions sufficient to yield an amount of said 2-quinoxalinecarboxylic acid. The present processes optionally further comprise the isolation and purification of 2-quinoxalinecarboxylic acid.

Microbial conversion of 2-methylquinoxaline

This invention provides a compound of formula (I):

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East Lyme, CT, United States of America

John Wing Wong