发明名称 |
PROCESS FOR THE SYNTHESIS OF AZETIDINONES |
摘要 |
This invention provides a process for preparing the hypocholesterolemic compound (I) comprising: (a) reacting p-fluorobenzoylbutyric acid with pivaloyl chloride and acylating the product with a chiral auxiliar y to obtain a ketone of formula (IV); (b) reducing the ketone of formula (IV) in the presence of a chiral catalyst to an alcohol; (c) reacting the chiral alcohol of step (b), an imine and a silyl protecting agent, then condensing the protected compounds to obtain a .beta. - (substituted-amino)amide of formula (VII); (d) cyclizing the .beta.-(substituted-amino)amide of formula (VII) with a silylating agent and a fluoride ion catalyst to obtain a protected lactam of formula (VIII); and removing the protecting groups. The intermediates of formulas (V II and VIII) are also claimed.
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申请公布号 |
CA2353981(C) |
申请公布日期 |
2005.04.26 |
申请号 |
CA19992353981 |
申请日期 |
1999.12.06 |
申请人 |
SCHERING CORPORATION |
发明人 |
COLON, CESAR;FU, XIAOYONG;MCALLISTER, TIMOTHY L.;THIRUVENGADAM, TIRUVETTIPURAM K.;CHIU, JOHN S.;TANN, CHOU-HONG |
分类号 |
C07D205/08;C07B61/00;C07F7/18;(IPC1-7):C07D205/08 |
主分类号 |
C07D205/08 |
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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