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The first efficient palladium(0)-catalyzed enantioselective C(sp 3 )-H activation reaction using a catalytic chiral base and an achiral phosphine ligand is reported. Fine-tuning the binol-derived phosphoric acid pre-catalyst and the reaction conditions was found to be crucial to achieve high levels of enantioselectivity for a variety of indoline products containing both tri- and tetrasubstituted stereocenters.

Palladium(0)-catalyzed asymmetric C(sp3)–H arylation using a chiral binol-derived phosphate and an achiral ligand

Palladium(0)-catalyzed asymmetric C(sp³)–H arylation using a chiral binol-derived phosphate and an achiral ligand