Application of polymer-bound 4-(bromomethyl)-3-nitrobenzoic acid for synthesis of trisubstituted 1,4-benzodiazepine-2,3-diones |
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Authors: | Zhang Jinfang Lou Boliang Saneii Hossain |
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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 |
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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-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. |
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Keywords: | 1 4-benzodiazepin-2 3-dione intramolecular cyclization N-alkylation polymer-bound precursor scaffold solid-phase synthesis |
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