公开(公告)号：US4629701A

公开(公告)日：1986-12-16

申请号：US627093

申请日：1984-07-02

申请人： Akihiro Sakimae ,  Yuri Kagawa ,  Ryozo Numazawa ,  Hisao Onishi

发明人： Akihiro Sakimae ,  Yuri Kagawa ,  Ryozo Numazawa ,  Hisao Onishi

IPC分类号： C12P11/00 ,  C12P41/00

CPC分类号： C12P41/00 ,  C12P11/00

摘要： Organic carboxylic acid ester represented by the formula (II): ##STR1## wherein R.sub.1 is an alkyl, an aralkyl or an aryl group; R.sub.2 is an alkyl group; R.sub.3 is an alkyl group; n is 1 or 2, are synthesized in racemic form, and then the acid ester (II) is treated with a source containing enzyme capable of rearranging with or without asymmetrically hydrolyzing ester bond until either a d-form or 1-form optically active carboxylic acid ester represented by the formula (II) with or without the antipode acid thereof is produced.

摘要翻译： 由式（II）表示的有机羧酸酯：其中R 1是烷基，芳烷基或芳基; R2是烷基; R3是烷基; n为1或2，以外消旋形式合成，然后用含有酶的酶处理酸酯（II），其能够或不具有不对称水解的酯键重排，直到d型或1-型光学活性羧基 制备了具有或不具有对映体酸的由式（II）表示的酸酯。

公开(公告)号：US5476791A

公开(公告)日：1995-12-19

申请号：US243521

申请日：1994-05-16

申请人： Akihiro Sakimae ,  Yuri Kagawa ,  Ryozo Numazawa ,  Hisao Onishi

发明人： Akihiro Sakimae ,  Yuri Kagawa ,  Ryozo Numazawa ,  Hisao Onishi

IPC分类号： C07D207/16 ,  C07D277/06 ,  C12P7/40 ,  C12P41/00 ,  C12P9/00

CPC分类号： C12P7/40 ,  C07D207/16 ,  C07D277/06 ,  C12P41/005 ,  Y10S435/822

摘要： N-(3-acetylthio-2-D-methylpropionyl)-L-proline useful as a precursor of captopril, one of antihypertensive agents, is prepared by allowing thioacetic acid to react with methyl methacrylate to prepare racetalc methyl 3-acetylthio-2-DL-methylpropionate, contacting the propionate with cells of, for example, Pseudomonas in order to effect biological and asymmetric hydrolysis, extracting 3-acetylthio-D-2-methylpropionic acid and allowing the acid to react with L-proline.

摘要翻译： 通过使硫代乙酸与甲基丙烯酸甲酯反应制备N-乙酰基-3-乙酰硫基-2-脯氨酸，其是抗高血压药之一，可用作卡托普利前体的N-（3-乙酰硫基-2-D-甲基丙酰基）-L-脯氨酸， DL-甲基丙酸酯，使丙酸酯与例如假单胞菌的细胞接触以进行生物和不对称水解，提取3-乙酰硫基-D-2-甲基丙酸，并使酸与L-脯氨酸反应。