Process for direct isolation of captopril

Details Process for direct isolation of captopril Process for direct isolation of captopril

C - Chemistry, Metallurgy

07

D

260/325.1

C07D 207/16 (2006.01)

Patent

CA 2027377

HA489 Abstract PROCESS FOR DIRECT ISOLATION OF CAPTOPRIL A process is disclosed for direct isolation of captopril from a substrate of the formula Image wherein R is lower alkyl or lower alkoxy. In this process, the substrate is first treated with an aqueous alkali metal hydroxide capable of forming a water-soluble salt of the substrate, wherein the alkali metal hydroxide has a concentration of 4 M or greater. The substrate is then neutralized, preferably with a mineral acid. By this process, captopril may be directly crystallized from an aqueous solution, avoiding the prior art use of organic solvents and zinc treatment to reduce levels of sulfide and disulfide impurities, respectively. In an alternative embodiment, neutralization is carried out by use of a hydrogen-supplying ion exchange resin.

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