发明名称 Novel method for the synthesis of perindopril and the pharmaceutically-acceptable salts thereof
摘要 <p>Disclosed is a process for industrial synthesis of the compound formula (I) and its pharmaceutically acceptable salts, characterised in that a compound of formula (II) wherein R1 represents a benzyl or linear or branched (C1-C6)alkyl group, is reacted with a compound of formula (III) having the S configuration wherein X represents a halogen atom and R2 represents a protecting group for the amino function, in the presence of a base to yield after deprotection of the amino function, a compound of formula (IV) wherein R1 is as defined hereinbefore, which is reacted with ethyl 2-oxopentanoate under hydrogen pressure, in the presence of platinum-on-carbon to yield a compound of formula (V) wherein R-1 is as defined hereinbefore, which is deprotected to yield the compound of formula (I).</p>
申请公布号 NZ545338(A) 申请公布日期 2009.03.31
申请号 NZ20040545338 申请日期 2004.08.27
申请人 LES LABORATOIRES SERVIER 发明人 DUBUFFET, THIERRY;LECOUVE, JEAN-PIERRE
分类号 C07K5/02;C07K5/06;(IPC1-7):C07K5/06;C07D209/42 主分类号 C07K5/02
代理机构 代理人
主权项
地址