Process for the preparation of high purity perindopril

Details Process for the preparation of high purity perindopril Process for the preparation of high purity perindopril

2007-10-09

2007-10-09

Saeed, Kamal A. (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acids and salts thereof

C562S433000

Reexamination Certificate

active

11788454

ABSTRACT:
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 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).The compound of the Formula I—perindopril—is a known ACE inhibitor.

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Harfenist, et al., Journal of Organic Chemistry, vol. 50, pp. 1356-1359, especially p. 1356.
Vincent, et al.,Drug Design and Discovery, 1992, 9, 11-28.
Vincent, M., et al., “Synthesis and Ace Inhibitory Activity of the Stereoisomers of Perindopril (S9490) and Perindoprilate (S 9780)” Drug Design and Discovery, Hardwood Academic Publishers GmbH, vol. 9, No. 1, 1992, pp. 11-28 XPOOO885876 ISSN: 1055-9612, p. 11-p. 13.

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