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filingDate 1997-04-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2000-02-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-008756-A1
titleOfInvention ENZYMATIC PROCESS FOR THE STEREOSELECTIVE PREPARATION OF THERAPEUTIC AMIDES
abstract A method of preparing an optically active compound of formula I where E is selected from nitrogen and CZ, where C is a ring carbon and Z is a substituent as defined below, where: when E is CZ, X and Z are selected of the group consisting of: (A) X is ArY where Y is a bond group selected from carbonyl, sulfinyl and sulfonyl and Ar is selected from the group consisting of phenyl substituted with 0-2 substituents selected from halo, hydroxy, C1-C4 cyano alkyl, and C1-C4 alkoxy; six-membered heteroaryl rings containing 1-2 nitrogen atoms as the sole heteroatoms, five-membered heteroaryl rings containing 1-2 heteroatoms selected from nitrogen, oxygen, and sulfur; and Z is selected from hydrogen, cyano, halo, hydroxy, C1-C4 alkyl and C1-C4 alkoxy; and (B) X is cyano and Z is selected from the group consisting of phenylthio, phenylsulfinyl, and phenylsulfonyl whose phenyl rings are substituted with 0-2 substituents selected from halo, hydroxy, cyano, nitro, C1-C4 alkyl, and C1-C4 alkoxy, and when E is nitrogen, X is independently selected from any of the aforementioned values of X (A); and * is an optically active chiral center, comprising the step of treating a racemic compound of formula II where X and E are as defined above and R1 is alkyl optionally substituted by one or more substituents independently selected from hydroxy, halogen, C1-C4 alkoxy, cyano, C1-C4 alkylamino and C1-C4 with a hydrolase enzyme. The invention also provides useful chiral intermediates to prepare the compound of formula I and enzymatic processes to prepare said chiral intermediates.
priorityDate 1996-04-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 53.