Simple process for producing high-quality captopril

Details Simple process for producing high-quality captopril Simple process for producing high-quality captopril

C - Chemistry, Metallurgy

07

D

C07D 207/16 (2006.01)

Patent

CA 2249543

An extremely simple process in which by-product impurities difficult to remove by purification are prevented from generating and high-quality captopril, represented by formula (1), can be inexpensively produced in a high yield. The process comprises hydrolyzing a substrate represented by general formula (2) (wherein R represents alkyl or alkoxyl) in an aqueous medium to eliminate the RCO group and then isolating the reaction product. The hydrolysis is conducted in the presence of a strong acid at 40 ~C or higher and a pH of 1 or lower.

Procédé extrêmement simple qui empêche la génération d'impuretés sous forme de sous-produits difficiles à enlever par purification et qui assure la production à haut rendement et à peu de frais du captotril de qualité supérieure répondant à la formule (1). Le procédé consiste à hydrolyser dans un milieu aqueux un substrat qui répond à la formule générale (2), où R représente un alkyle ou un alcoxyle, afin d'éliminer le groupe RCO et d'isoler ainsi le produit de la réaction. L'hydrolyse est menée en présence d'un acide fort à une température égale ou supérieure à 40 ·C et avec un pH égal ou inférieur à 1.

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