Molecular Diversity 2003-01-01

Application of polymer-bound 4-(bromomethyl)-3-nitrobenzoic acid for synthesis of trisubstituted 1,4-benzodiazepine-2,3-diones.

Jinfang Zhang, Boliang Lou, Hossain Saneii

Index: Mol. Divers. 6(1) , 13-7, (2003)

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Abstract

A method utilizing polymer-bound 4-(bromomethyl)-3-nitrobenzoic acid as a key precursor leading to 1,4-benzodiazepin-2,3-dione scaffold is described. It involves a four-step sequence including nucleophilic displacement, acylation, simultaneous reduction-cyclization and alkylation, providing rapid access to the title compounds in excellent yield and purity.