Process for the preparation of high purity perindopril and...

C - Chemistry – Metallurgy – 07 – D

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C07D 209/42 (2006.01) A61K 31/404 (2006.01) A61P 9/12 (2006.01) C07C 271/22 (2006.01)

Patent

CA 2474003

The invention relates to 1-{2(S)-[1(S)-(ethoxycarbonyl)butylamino]propionyl}- (3aS,7aS)octahydroindol-2(S)-carboxylic acid of the Formula I and the t- butylamine salt of the Formula I' thereof (see formula I) (see formula I') free of contaminations derivable from dicyclohexyl carbodiimide, and a process for the preparation thereof. The invention also relates to new intermediates of the general Formula III (wherein R stands for lower alkyl or aryl lower alkyl). (see formula III) The compound of the Formula I - perindopril - is a known ACE inhibitor.

L'invention concerne un acide 1-{2(S)-[1(S)-(éthoxycarbonyl)butylamino]propionyl}-(3aS,7aS)octahydroindol-2(S)-carboxylique de formule (I) ainsi que le sel de t-butylamine de formule (I') correspondant, ces composés ne contenant pas de contaminants dérivables du dicyclohexyle carbodiimide. L'invention concerne également un procédé de préparation correspondant ainsi que des nouveaux produits intermédiaires de formule générale (III) (dans laquelle R représente alkyle inférieur ou arylalkyle inférieur). Le composé de formule (I), soit le périndopril, est un inhibiteur ECA connu.

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