<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
DE69925862(D1)
申请公布日期
2005.07.21
申请号
DE1999625862
申请日期
1999.12.06
申请人
SCHERING CORP., KENILWORTH
发明人
THIRUVENGADAM, TIRUVETTIPURAM K.;FU, XIAOYONG;TANN, CHOU-HONG;MCALLISTER, TIMOTHY L.;CHIU, JOHN S.;COLON, CESAR