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

2018-11-28T14:45:36Z (GMT) by Junjie Chen Xiuling Han Xiyan Lu
A Pd­(OAc)<sub>2</sub>-catalyzed asymmetric cyclization of 2-aminoaryl alkynones involving an intramolecular <i>trans</i>-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.