An efficient synthesis of benzodiazepinyl phosphonates as clostripain inhibitors via FeCl3 catalyzed four-component
Asish K Bhattacharya1, Kalpeshkumar C Rana, Dnyaneshwar S Raut
1Division of Organic Chemistry, National Chemical Laboratory (NCL-CSIR), Dr Homi Bhabha Road, Pune 411 008, India. ak.bhattacharya@ncl.res.in
Abstract:
A novel one-pot route for the synthesis of benzodiazepinyl phosphonates (BDPs) has been achieved. FeCl(3) 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.
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