Synlett 2014; 25(07): 939-944
DOI: 10.1055/s-0033-1340837
letter
© Georg Thieme Verlag Stuttgart · New York

A Trifluoroacetic Acid Catalyzed Domino Reaction as an Approach to Amino Acid Derived 2,3-Dihydro-1H-1,5-benzodiazepines

Saurav Bera
a   Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226031, UP, India   Email: gautam.panda@gmail.com   Email: gautam_panda@cdri.res.in
,
Pancham S. Kandiyal
b   Sophisticated Analytical Instrumental Facility Division, CSIR-Central Drug Research Institute, Lucknow 226031, UP, India
,
Ravi S. Ampapathi
b   Sophisticated Analytical Instrumental Facility Division, CSIR-Central Drug Research Institute, Lucknow 226031, UP, India
,
Gautam Panda*
a   Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226031, UP, India   Email: gautam.panda@gmail.com   Email: gautam_panda@cdri.res.in
› Author Affiliations
Further Information

Publication History

Received: 14 December 2013

Accepted after revision: 28 January 2014

Publication Date:
11 March 2014 (online)


This paper is dedicated to Prof. M. Periasamy on his 60th birthday.

Abstract

Trifluoroacetic acid catalyzed condensation of aromatic amines with substituted benzaldehydes followed by intramolecular cyclization furnishes a highly effective synthesis of amino acid derived 2,3-dihydro-1H-1,5-benzodiazepines. The strategy provides an efficient access to a library of benzodiazepines that can be explored for potential pharmaceutical or biological activities.

Supporting Information