Enantioselective functionalization of prochiral C-H bonds is a highly attractive strategy for the construction of chiral compounds.Despite extensive efforts[1],enantioselective C(sp~3)-H functionalization still remains challenging at present.For instance,although enantioselective C-H functionalization via desymmetrization of two carbon centers has been accomplished with Pd catalysis and a directing group,differenciation of the prochiral C-H bonds on one methylene carbon center has rarely been achieved.On a different front,introduction of a transient chiral directing group is expected to be useful in enantioselective C-H arylation of C(sp~2)-H bonds.Nevertheless,transient amino acid directing group is Enantioselective functionalization of prochiral CH bonds is a highly attractive strategy for the construction of chiral compounds. Despite extensive efforts [1], enantioselective C (sp ~ 3) -H functionalization still remains at present. For instance, although enantioselective CH functionalization via desymmetrization of two carbon centers has been accomplished with Pd catalysis and a directing group, differeniation of the prochiral CH bonds on one methylene carbon center has rarely been achieved. On a different front, introduction of a transient chiral directing group is expected to be useful in enantioselective CH arylation of C (sp ~ 2) -H bondss.Nevertheless, transient amino acid directing group is