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Solid-phase synthesis of tetrahydro-1,4-benzodiazepin-2-one derivatives |
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| Authors: | Zhang Jinfang Goodloe Wesley P Lou Boliang Saneii Hossain |
| Institution: | Department of Chemistry, Advanced SynTech, 9800 Bluegrass Parkway, Louisville, KY 40299, USA. |
| Abstract: | An efficient method for solid-phase construction of tetrahydro-1,4-benzodiazepin-2-one scaffold is described. Polymer-bound 4-(bromomethyl)-3-nitrobenzoic acid was reacted with alpha-amino acid methyl esters, followed by nitro group reduction and hydrolysis. Subsequent intramolecular cyclization and alkylation at N(4) afforded the structurally diverse products in high yields and excellent purities. |
| Keywords: | benzodiazepine combinatorial chemistry intramolecular cyclization polymer-bound precursor scaffold solid-phase synthesis |
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