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.

The given article describes the synthesis of 2-Oxazolidinone ring via proline catalyzed stereoselective α-aminoxylation of aldehyde. 2-Oxazolidinone ring is a common core structure during the synthesis of oxazolidinones class molecules. Using this simple, facile and efficient methodology, Linezolid andsutezolid were prepared using asymmetric catalysis.

Selective α-aminoxylation was achieved on corresponding aldehyde with great enantiomeric excess to get intermediate (5) using catalytic amount of low cost proline. The oxazolidinone ring was then constructed on common intermediate (5) which was then further converted to Oxazolidinone class compounds like Sutezolid and Eperezolid.