发明名称 |
Process for the preparation of esters of 4-(2,3-epoxypropoxy)phenylacetic acid and 4-(2-hydroxy-3-isopropylamino-propoxy)phenylacetic acid and/or atenolol in stereospecific form. |
摘要 |
<p>S-(-)-atenolol (4-(2-hydroxy-3-isopropylaminopropoxy)phenyl acetamide) is obtained by a process including the step of stereo-specific epoxidation by an ester of 4-allyloxyphenylacetic acid using a micro-organism capable of stereo-selective epoxidation, e.g. Pseudomonas oleovorans, to produce the corresponding ester of 4-(2,3-epoxypropoxy)phenylacetic acid which is predominantly in S configuration. Pseudomonas oleovorans ATCC 29347 produces at least about 90% of the epoxypropoxy compound in S configuration. The resulting epoxypropoxy compound can be converted into atenolol, maintaining the high proportion of S configuration, by reacting the epoxypropoxy compound with isopropylamine and converting the ester group to an amide group by reaction with ammonia.</p> |
申请公布号 |
EP0256586(A1) |
申请公布日期 |
1988.02.24 |
申请号 |
EP19870201434 |
申请日期 |
1987.07.24 |
申请人 |
GIST-BROCADES N.V.;SHELL INTERNATIONALE RESEARCH MAATSCHAPPIJ B.V. |
发明人 |
PHILLIPS, GARETH THOMAS;BERTOLA, MAURO ATTILIO;MARX, ARTHUR FRIEDRICH;KOGER, HEIN SIMON |
分类号 |
C07D301/02;C07D303/22;C12P17/02;C12R1/38;(IPC1-7):C07C103/30;C07C93/00;C07C102/00 |
主分类号 |
C07D301/02 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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