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Palladium(II)-Catalyzed Asymmetric Tandem Cyclization of 2‑Aminoaryl Alkynones: An Approach to Chiral 1,2,3,4-Tetrahydro-β-carbolines

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journal contribution
posted on 2018-11-28, 14:45 authored by Junjie Chen, Xiuling Han, Xiyan Lu
A Pd­(OAc)2-catalyzed asymmetric cyclization of 2-aminoaryl alkynones involving an intramolecular trans-aminopalladation of alkyne and 1,2-addition to the carbonyl group tandem processes was developed. This strategy represents the first example using palladium as the catalyst and 2-alkynylaniline derivatives as the starting material to allow facile access to chiral 1,2,3,4-tetrahydro-β-carbolines in high yields and excellent enantioselectivities.

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