Three‐Component 1,4‐Addition through Ugi‐Type Reaction, an Oxidative Dearomatization Strategy

Abstract A three‐component 1,4‐addition variant of the Ugi reaction involving carboxylic acids, isocyanides, and cyclic α,β‐unsaturated imines is presented in this study. The cyclic α,β‐unsaturated imines were conveniently prepared through the oxidative dearomatization of N ‐substituted anilines. The reaction proceeded successfully to produce a sole diastereomer, and the relative configuration was determined through 2D NMR and X‐ray diffraction analysis.