Novel Cu(I)-catalyzed one-pot multicomponent synthesis of the antiepileptic drug rufinamide

摘要

This work represents a new synthesis of the antiepileptic drug rufinamide, through a one-pot multicomponent approach employing a Cu(I) as a catalyst. In this methodology, 2,6-difluoro benzyl bromide reacts with NaN3 and propiolamide in the presence of 0.5 mol% [Cu(phen)(PPh3)(2)]NO3 as a catalyst under click condition to afford regioselectively rufinamide in 95% yield. The new protocol offers several advantages such as high yields, clean reaction profile, short reaction time, use of less toxic catalyst, environmentally friendly and one pot approach.