Issue 15, 2011

An efficient synthesis of benzodiazepinyl phosphonates as clostripain inhibitorsviaFeCl3 catalyzed four-component reaction

Abstract

A novel one-pot route for the synthesis of benzodiazepinyl phosphonates (BDPs) has been achieved. FeCl3 efficiently catalyzed four-component condensation of diamines, acetone and phosphites in the presence of molecular sieves to furnish BDPs as novel chemical entities with good yield. The synthesized BDPs have shown significant protease inhibition activity against clostripain, a disease model for gas gangrene, suggesting that these novel chemical entities could be further explored as cysteine protease inhibitors.

Graphical abstract: An efficient synthesis of benzodiazepinyl phosphonates as clostripain inhibitorsviaFeCl3 catalyzed four-component reaction

Supplementary files

Article information

Article type
Paper
Submitted
01 Dec 2010
Accepted
29 Mar 2011
First published
30 Mar 2011

Org. Biomol. Chem., 2011,9, 5407-5413

An efficient synthesis of benzodiazepinyl phosphonates as clostripain inhibitorsviaFeCl3 catalyzed four-component reaction

A. K. Bhattacharya, K. C. Rana, D. S. Raut, V. P. Mhaindarkar and M. I. Khan, Org. Biomol. Chem., 2011, 9, 5407 DOI: 10.1039/C0OB01102A

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