Solid-phase synthesis of tetrahydro-1,4-benzodiazepin-2-one derivatives
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Updated: Sep 29, 2026

Preparation of N-(2-alkoxyvinyl)sulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
1Department 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.
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