发明名称 |
PROCESS FOR THE SYNTHESIS OF AZETIDINONES |
摘要 |
<p>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 auxiliary 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 (VII and VIII) are also claimed.</p> |
申请公布号 |
EP1137634(A1) |
申请公布日期 |
2001.10.04 |
申请号 |
EP19990963973 |
申请日期 |
1999.12.06 |
申请人 |
SCHERING CORPORATION |
发明人 |
THIRUVENGADAM, TIRUVETTIPURAM K.;FU, XIAOYONG;TANN, CHOU-HONG;MCALLISTER, TIMOTHY L.;CHIU, JOHN S.;COLON, CESAR |
分类号 |
C07D205/08;C07B61/00;C07F7/18;(IPC1-7):C07D205/08 |
主分类号 |
C07D205/08 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|