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

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.