In Gaunts and Yus works, some derivatives of drug molecules and biologically active compounds were successfully functionalized in their meta-position. For instance, meta-arylated derivatives of anti-inflammatory drugs (S)-ibruprofen and (S)-naproxen were synthesized with copper catalyzed C–H arylation. Meta-olefinated biologically important biphenyl, amino acid and Baclofen derivatives have been accessed by remote C–H activation assisted by the "end-on" template. These demonstrate the potential applications of meta-selective C–H functionalization in medicinal chemistry.