Highly Diastereoselective Synthesis of 1-Carbamoy1-4-aminoindoloazepinone Derivatives via the Ugi Reaction

Subtitle:IF 6.324

Abstract

A one-pot procedure for the highly diastereoselective synthesis of 1-carbamoy1-4-amino-1,2,4,5-tetrahydroindolo[2,3-c]azepin-3-one derivatives is described. Using 2-formyk-tryptophan as a bifunctional building block, a catalyst-free Ugi-three-component reaction (Ugi-3CR) was developed to present trisubstituted indoloazepinones in good yields and excellent diastereomeric excess.

Publication year:2013

Keywords:stereoselective 4-component condensations, multicomponent reactions, drug discovery, isosyanides, alpha, chemistry, potent, construction, antagonists, lactams