Herein, we have described a novel and concise synthesis of the potent angiotensin-convertingenzyme (ACE) inhibitor, benazepril hydrochloride (7) in trifluoroethanol via an Ugi three-component reactionin shorter reaction times. The key step is the trifluoroacetic acid-mediated hydrolysis of secondary amides (4aand 4b) followed by esterification as a domino process to form corresponding ethyl ester (6). Mainly twouniversal convertible isocyanides (1a and 1b) were used for the synthesis of benazepril hydrochloride.
Synopsis: An efficient synthesis of benazepril hydrochloride using Ugi three-component reaction.
Volume 133, 2021
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