simple and efficient method for the synthesis of wide range of 3,3-dimethyl-11-alkyl or aryl 2,3,4,5-tetrahydro-1H-dibenzo[b,e][1,4]diazepin-1-ones, recently reported as hepatitis C virus (HCV) NS5B polymerase inhibitors, is presented. The proposed method consists of one-pot condensation between 1,2-phenylenediamine and 5,5-dimethylcyclohexane-1,3-dione (dimedone) followed by cyclization with various alkyl and aryl acyl chlorides catalyzed by Er(III) triflate. With respect to methods previously reported, the proposed one-pot procedure furnishes appreciably higher yield of product in shorter reaction time.

One-Pot Synthesis of Dibenzo[b,e][1,4]diazepin-1-ones

DE NINO, Antonio;
2012

Abstract

simple and efficient method for the synthesis of wide range of 3,3-dimethyl-11-alkyl or aryl 2,3,4,5-tetrahydro-1H-dibenzo[b,e][1,4]diazepin-1-ones, recently reported as hepatitis C virus (HCV) NS5B polymerase inhibitors, is presented. The proposed method consists of one-pot condensation between 1,2-phenylenediamine and 5,5-dimethylcyclohexane-1,3-dione (dimedone) followed by cyclization with various alkyl and aryl acyl chlorides catalyzed by Er(III) triflate. With respect to methods previously reported, the proposed one-pot procedure furnishes appreciably higher yield of product in shorter reaction time.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11770/134246
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