Rh(III)-catalyzed C(sp2)H arylation and esterification cascade reaction of aryl acids with organic boronates

Herein, we have successfully developed an efficient catalytic protocol to proceed the arylation/esterification cascade reaction of aryl carboxylic acids with aromatic boronates. This catalytic methodology was compatible with various substrates and coupling partners well. This catalytic protocol could proceed the late-stage modification of roflumilast precursor, which offered the potential application of developing novel drug molecules.