Bristol-myers Squibb Compnay

Brenda Joyce White

Paul M Skonezny

Li You

Ramesh N Patel

Ronald L Hanson

Jingyang Zhu

Michael Politino

Jason G Chen

David B Brzozowski

Iqbal Gill

Francisco Moris-Varas

John J Usher

Shannon X Zhao

Jiri Novotny

Shannon X Zha

An enzymatic ammonolysis process is provided for the preparation of intermediates used in preparing dipeptidyl peptidase IV inhibitors wherein the enzymelipase-B is used to catalyze the ammonolysis process.

Enzymatic ammonolysis process for the preparation of intermediates for DPP IV inhibitors

Provided is a method of resolving a racemic mixture of a compound of formula I to obtain a desired enantiomer:wherein Ar is Cor Caromatic group that can be substituted with H, Cto Calkyl, trifluoromethyl or halo, Ris halo or &#x2014;S&#x2014;R, wherein Ris H or acetyl, and Ris H or Cto Calkyl, the method comprising: reacting a compound of formula I wherein the compound is an ester whereby Ris Cto Calkyl with a lipase derived fromto stereoselectively hydrolyze the ester bond to produce an acid; and isolating the acid, wherein the reaction is conducted in a solvent comprising 80% to 98% v/v % organic phase and a residue of water phase (which can be buffered).

Enzymatic resolution of aryl and thio-substituted acids

New mutant penicillin G acylases preferably from are provided, exhibiting altered enzymatic activity. These penicillin G acylases are obtained by expression of a gene encoding said penicillin G acylase having an amino acid sequence which differs at least in one amino acid from the wild-type penicillin G acylase.

Mutant penicillin G acylases

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Jamesville, NY, United States of America

Brenda Joyce White