Diversification of pharmaceutical molecules via late-stage C(sp2)–H functionalization

C–H late-stage functionalization has gradually become a powerful approach for the rapid optimization of lead compounds' bioactivity. Significant advances in this field have been achieved in the past few years, mainly, the C–H functionalization system in (hetero)aryl C–H activation owing to the importance of (hetero)aryl moiety in pharmaceutical. In this review, we described the selected recent examples of how developed intermolecular C(sp2)–H functionalization methodologies involving diverse techniques diversify pharmaceutical molecules in the late stage.