Synthesis of 2-substituted tryptophans via a C3- to C2-alkyl migration

Beilstein J Org Chem. 2014 Aug 26:10:1991-8. doi: 10.3762/bjoc.10.207. eCollection 2014.

Abstract

The reaction of 3-substituted indoles with dehydroalanine (Dha) derivatives under Lewis acid-mediated conditions has been investigated. The formation of 2-substituted tryptophans is proposed to occur through a selective alkylative dearomatization-cyclization followed by C3- to C2-alkyl migration and rearomatization.

Keywords: Dehydroalanine; Friedel–Crafts alkylation; indoles; migration; tryptophans.