发明名称 |
Verfahren zur Synthese des (2S,3aS,7aS)-perhydroindol-2-carbonsäures und seiner Estern, Verwendung in der Synthese von Perindopril |
摘要 |
<p>Production of (2S,3aS,7aS)-perhydroindole-2-carboxylic acid derivatives (I) comprises reacting 1-(1-cyclohexenyl)pyrrolidine (III) with a N-protected 3-iodoalanine derivative (IV), deprotecting the amino group, cyclizing and dehydrating the product, catalytically hydrogenating the product at 1-30 bar, and optionally deprotecting or reprotecting the acid group. Production of compounds of formula (I) comprises reacting 1-(1-cyclohexenyl)pyrrolidine (III) with a N-protected 3-iodoalanine compound of formula (IV) to give a product of formula (V), deprotecting the amino group and cyclizing and dehydrating the product to give a compound of formula (VI), and catalytically hydrogenating (VI) at 1-30 bar and optionally deprotecting or reprotecting the acid group. R = H or a protecting group, and R' = a protecting group. An Independent claim is also included for production (unspecified) of perindopril or its salts from (I) produced as above.</p> |
申请公布号 |
DE60301980(D1) |
申请公布日期 |
2005.12.01 |
申请号 |
DE2003601980 |
申请日期 |
2003.02.28 |
申请人 |
LES LABORATOIRES SERVIER, COURBEVOIE |
发明人 |
DUBUFFET, THIERRY;LANGLOIS, PASCAL |
分类号 |
C07D209/42;(IPC1-7):C07D209/42 |
主分类号 |
C07D209/42 |
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