发明名称 |
PROCESS FOR PRODUCING 3,4-DISUBSTITUTED PYRROLIDINE DERIVATIVE AND PRODUCTION INTERMEDIATE THEREOF |
摘要 |
An industrially advantageous process for the production of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof that is useful as an intermediate for the production of novel antimicrobial agents 10-(3-cyclopropylaminomethyl-4-fluoropyrrolidinyl)pyridobenzox azine carboxylic acid derivatives. Highly stereoselective asymmetric hydrogenation of 1-protected-4-alkoxycarbonyl-3-oxopyrrolidine, followed by ester hydrolysis, followed by amidation with cyclopropylamine gives crude crystals. The crude crystals are purified by recrystallization to give a novel compound. (3R,4S)-1-protected-3-cyclopropylcarbamoyl-4-hydroxypyrrolidin e or an enantiomer thereof at high optical purity. The use of these intermediates enables industrial production of high-quality products of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof. The process is highly simple and can produce the desired products at high purity and stable yields. |
申请公布号 |
CA2645191(C) |
申请公布日期 |
2014.05.06 |
申请号 |
CA20072645191 |
申请日期 |
2007.03.08 |
申请人 |
KYORIN PHARMACEUTICAL CO., LTD. |
发明人 |
GOTOH, TAKAYUKI;ARAYA, ICHIROU |
分类号 |
C07D207/10;C07B61/00;C07D207/16 |
主分类号 |
C07D207/10 |
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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