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The application of an electron-deficient pyridone ligand can be important for the observed large enantioselectivity. Interestingly, using different gold salts can reverse the enantioselectivity into the C( sp 3 )-H arylation reaction. These crucial mechanistic results will give you insight for future development of Pd(II)-catalyzed enantioselective C( sp 3 )-H activation reactions with chiral TDGs. © 2020 WILEY-VCH Verlag GmbH Co. KGaA, Weinheim.Sphingosine-1-phosphate (S1P) is a normal bioactive lip