Abstract

Main observation and conclusionA highly efficient kinetic resolution of racemic 2‐substituted 1,2‐dihydroquinolines via Rh‐catalyzed asymmetric hydroarylation has been described for the first time. A variety of arylboronic acids coupled with 2‐substituted 1,2‐dihydroquinolines under mild reaction condition. The transformations into the enantio‐enriched 2,3‐diaryl‐tetrahydroquinolines as well as the recovered chiral 2‐aryl‐dihydroquinolines were obtained with high yields and excellent enantioselectivities (86%—99% ee, s factor up to 1057).

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