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      Permanent link:
      https://www.ias.ac.in/article/fulltext/jcsc/133/0035

    • Keywords

       

      Ugi reaction; convertible isocyanides; a-amino amide; esterification.

    • Abstract

       

      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.

    • Graphical Abstract

       

      Synopsis: An efficient synthesis of benazepril hydrochloride using Ugi three-component reaction.

    • Author Affiliations

       

      BHUSHAN B BORASE1 HIMANSHU M GODBOLE1 GIRIJ P SINGH1 PRITESH R UPADHYAY1 ANURAG TRIVEDI1 VARADARAJ BHAT2 GAUTHAM G SHENOY2

      1. Research and Development, Lupin Limited, Mulshi, India
      2. Manipal Academy of Higher Education, Manipal, India

    • Dates

       
      Published
      7 April 2021
      Manuscript received
      5 July 2020
      Manuscript revised
      6 December 2020
      Accepted
      3 January 2021

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