发明名称 PREPARATION OF ARYLGLYCIDYL ETHERS AND 3-SUBSTITUTED 1-ALKYLAMINO -2- PROPANOLS
摘要 A process for the preparation of a pharmaceutically active compound in a stereospecific form of the formula R1-O-CH2-CHOH-CH2-NH-R2 (I) or a pharmaceutically acceptable salt thereof, like an acid addition salt, and/or a compound in a stereospecific form of the formula <CHEM> wherein R1 is an optionally substituted aryl group including a phenyl or naphthyl group optionally included in a heterocyclic ring system, which is optionally substituted, or is a heteroaromatic 5 or 6 membered ring containing in addition to carbon atoms, one or more atoms selected from nitrogen, sulphur and oxygen, this ring being optionally substituted, and wherein R2 is an alkyl group of 2 to 6 carbon atoms, this alkyl group being optionally substituted, which comprises subjecting a compound of the formula R1-O-CH2-CH=CH2 (III) to the action of a micro-organism having the ability for stereoselective epoxidation of compound (III) into compound (II), having at least 80% by weight the S configuration, at least partly separating compound (II) and/or reacting compound (II) with a C2-C6 alkylamine group optionally substituted and at least partly separating compound (I) and/or converting compound (I) into the pharmaceutically acceptable salt thereof.
申请公布号 AU5327086(A) 申请公布日期 1987.04.30
申请号 AU19860053270 申请日期 1986.02.06
申请人 GIST-BROCADES NV, SHELL INTERNATIONALE RESEARCH MAATSCHAPPIJ;B.V. 发明人 GARETH THOMAS PHILLIPS;BRIAN WILLIAM ROBERTSON;MAURO ATTILIO BERTOLA;HEIN SIMON KOGER;ARTHUR FRIEDRICH MARX;DOUGLAS PETER WATTS
分类号 C07D301/02;C07D303/22;C07D303/24;C12P17/02 主分类号 C07D301/02
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