Diastereoselective Access to 3-Aminoindanones Through Domino Approach

A unique intermolecular approach for stereoselective synthesis of 3-aminoindanones bearing a β-quaternary carbon from 2-alkynylacetophenones and anilines has been reported. The catalytic system comprised of silver salt and phosphoric acid effectively transformed a range of 2-alkynylacetophenones and anilines to corresponding 3-aminoindanones in moderate to good yields with excellent diastereoselectivity and broad functional group tolerance. Furthermore, scale up and synthetic transformations were carried out to demonstrate the synthetic utility of the developed protocol.