3-Aminoindole Synthesis from 2-Nitrochalcones and Ammonia or Primary Amines

A step-economic strategy for 3-aminoindoles synthesis with ammonia or primary amines as N source under transition-metal-free conditions was achieved. A series of 3-aminoindoles was obtained with abundant N source featuring high efficiency, mild conditions, environmental friendliness and scalability. Efficient syntheses of the intermediates of COX-2 inhibitor and tubulin polymerization inhibitor were successfully accomplished with this newly developed strategy.