Solid-Phase Synthesis of Trisubstituted 2,5-Dihydrobenzo[<i>f</i>][1,2,5]thiadiazepine 1,1-Dioxide Derivatives

Abstract

The solid-phase synthesis of trisubstituted 2,5-dihydrobenzo[f][1,2,5]thiadiazepine 1,1-dioxides is reported. Acyclic polymer-supported intermediates were prepared using commercially available building blocks: Fmoc-protected amino acids, 2-nitrobenzenesulfonyl chlorides, and bromoketones. The acyclic precursors underwent acid-mediated release from the resin and the cyclization was completed in solution.