A simple route to morpholine derivatives via copper‐acetylide addition to carbodiimide in the presence of oxiranes

Abstract

A novel catalytic multicomponent reaction for the synthesis of morpholine derivatives has been reported. The reactions involve terminal alkynes, carbodiimides, and oxiranes using [Cu (CH 3 CN) 4 ]PF 6 , t BuOLi, and TBPAc in anhydrous NMP. Aryl and heteroaromatic terminal alkynes were tolerated.Carbodiimides could be symmetrical and unsymmetrical substrates with aryl or alkyl substituents. The reaction exhibited a good regioselectivity when unsymmetrical carbodiimides were employed.