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Application of polymer-bound 4-(bromomethyl)-3-nitrobenzoic acid for synthesis of trisubstituted 1,4-benzodiazepine-2,3-diones
Authors:Zhang  Jinfang  Lou  Boliang  Saneii  Hossain
Affiliation:(1) Department of Chemistry, Advanced SynTech, 9800 Bluegrass Parkway, Louisville, KY, 40299;(2) Department of Chemistry, Advanced SynTech, 9800 Bluegrass Parkway, Louisville, KY, 40299
Abstract:A method utilizing polymer-bound 4-(bromomethyl)-3-nitrobenzoic acid as a key precursor leading to 1,4-benzodiazepin-2,3-dionescaffold is described. It involves afour-step sequence including nucleophilic displacement,acylation, simultaneous reduction-cyclization and alkylation,providing rapid access to the title compounds in excellent yieldand purity.
Keywords:1  4-benzodiazepin-2  3-dione  intramolecular cyclization  N-alkylation  polymer-bound precursor  scaffold  solid-phase synthesis
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