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US 2006/0189813 A1Published application
Novel method for the synthesis of perinidopril and the pharmaceutically acceptable salts thereof
AssigneeLes Laboratories Servier
InventorsClaude Fugier, Thierry Dubuffet, Pascal Langlois
Life of this patent
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Abstract
Process for the synthesis of perindopril of formula (I): and its pharmaceutically acceptable salts.
Claims10
1-9. (canceled)
A process for the synthesis of a compound of formula (I):
- and its pharmaceutically acceptable salts,
- wherein a compound of formula (II):
- wherein R represents hydrogen, benzyl or linear or branched (C1-C6)alkyl, is reacted
- with a compound of formula (III) having the (R) configuration:
- wherein G represents chlorine, bromine, iodine, hydroxy, p-toluenesulphonyloxy, methanesulphonyloxy or trifluoromethanesulphonyloxy,
- in the presence of a base,
- to yield a compound of formula (IV):
- which is reacted with the compound of formula (V) having the (S) configuration:
- to yield a compound of formula (VI):
- which is hydrogenated in the presence of a catalyst,
- to yield, after deprotection where necessary, the compound of formula (I).
8 more elements
A compound selected from those of formula (IV):
- wherein R represents hydrogen, benzyl or linear or branched (C1-C6)alkyl and G represents chlorine, bromine, hydroxy, p-toluenesulphonyloxy, methanesulphonyloxy or trifluoromethanesulphonyloxy.
Dependencies are inferred from the claim text.