发明名称 STEREOSELECTIVE SYNTHESIS OF 2-HYDROXY-4-PHENYLBUTYRIC ACID ESTERS
摘要 <p>A process is described for the stereospecific preparation of an ester of formula (I): wherein *signifies the (R) stereoisomer; R<1> is selected from C1-6 alkyl, preferably ethyl; and R<2> is hydrogen, a protecting group or a leaving group which process comprises reaction of a nitrile of formula (II): wherein *signifies the (R) stereoisomer; and Ph is the phenyl group C6 H5 with a solution of an inorganic acid in an alcohol and optional conversion of the compound of formula (I) wherein R<2> is H so prepared to any other desired compound of formula (I) by standard methods in the art. The compounds of formula (I) are chiral esters, useful as intermediates in the synthesis of the family of acetylcholine esterase (ACE) inhibitors known as 'prils', such as lisinopril, cilazapril, enalapril, benazepril, ramipril, delapril, enalaprilat, imidapril, spirapril, trandolapril and others.</p>
申请公布号 WO02094761(A1) 申请公布日期 2002.11.28
申请号 WO2002IB01689 申请日期 2002.05.16
申请人 FERMENTA BIOTECH LTD;TIKARE, RAVEENDRA, KHANDURAO 发明人 TIKARE, RAVEENDRA, KHANDURAO
分类号 C07D487/04;C07B53/00;C07B61/00;C07C67/22;C07C69/732;(IPC1-7):C07C67/22;C07C229/36;C07C69/734 主分类号 C07D487/04
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