Weak, bidentate chelating group assisted cross-coupling of C(sp)-H bonds in aliphatic acid derivatives with aryltrifluoroborates.

A protocol of Pd(ii)-catalyzed, weak bidentate directing group assisted β-C(sp3)-H activation/cross-coupling with organoboron reagents has been achieved, affording arylation of aliphatic acid derivatives that contain α-hydrogen atoms in moderate to good yields. The potential of this method for an asymmetric β-C(sp3)-H arylation via desymmetrization was also presented.