Solid-phase synthesis of C-terminal azapeptides

Abstract

The solid-phase synthesis of azapeptides possessing a C-terminal aza-residue has been accomplished by a protocol featuring regioselective alkylation of benzhydrylidene-aza-glycinamide and illustrated by the syntheses of [aza-Lys(6)] growth-hormone-releasing peptide-6 analogs.

Keywords: C-terminal azapeptides; acylation of semicarbazide; benzhydrylidene-protecting group; regioselective alkylation.