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Issue 15, 2011
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An efficient synthesis of benzodiazepinyl phosphonates as clostripain inhibitorsviaFeCl3 catalyzed four-component reaction

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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

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Publication details

The article was received on 01 Dec 2010, accepted on 29 Mar 2011 and first published on 30 Mar 2011


Article type: Paper
DOI: 10.1039/C0OB01102A
Citation: Org. Biomol. Chem., 2011,9, 5407-5413

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    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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