Title: Process for preparing esters of 4-(2-hydroxy-3-isopropylamino-propoxy) phenylacetic acid and/or atenolol in stereospecific form
Application Number: 87105324 Application Date: 1987.08.17
Publication Number: 1031397 Publication Date: 1989.03.01
Approval Pub. Date: Granted Pub. Date: 1993.06.02
International Classifi-cation: C12P13/00,C12P17/02
Applicant(s) Name: Gist-Brocades N.V. Address:
Inventor(s) Name: Bertola Mauro Attilio, Marx Arthur Friedrich
Attorney & Agent: TIANG YUE
Abstract:
     A process is provided for the preparation of atenolol (4-(2-hydroxy-3-isopropylaminopropoxy)phenylacetamide) in a stereospecific form or a pharmaceutically acceptable salt thereof, and/or a stereospecific form of methyl-4-(2,3-epoxypropoxy) phenylacetate or methyl-4-(2-hydroxy-3-isopropylamino propoxy) phenylacetate which comprises subjecting 4-allyloxyphenylacetate to the action of a micro-organism having the ability for stereoselective epoxidation of 4-allyloxyphenylacetate into methyl-4-(2,3-epoxypropoxy) phenylacetate, having at least 80% by weight the S configuration, at least partly separating methyl-4-(2,3-epoxypropoxy) phenylacetate and/or reacting methyl-4-(2,3-epoxypropoxy) phenylacetate with isopropylamine, at least partly separating methyl-4-(2-hydroxy-3-isopropylamino propoxy) phenylacetate and/or reacting methyl-4-(2-hydroxy-3-isopropylaminopropoxy) phenylacetate with ammonia and at least partly separating atenolol and/or converting atenolol into the pharmaceutically.....
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