Direct and Efficient C(sp3)‐H Bond Alkylation of Tetrahydroisoquinolines and Isochroman with Alkylzinc Reagents

An efficient C(sp3)−H bond alkylation of tetrahydroisoquinolines and isochroman with alkylzinc reagents was demonstrated. This transformation could be readily performed under mild conditions in the absence of a heavy metal catalyst, affording a wide range of potentially biologically active compounds. In addition, this approach exhibited excellent compatibility with various sensitive functional groups such as a cyano group, an ester group as well as a boronic acid pinacol ester group.