Discovery of Plant Growth Stimulants by C–H Arylation of 2-Azahypoxanthine

A series of new AHX derivatives were synthesized by Pd-catalyzed C–H arylation. Their rice-growth-promoting activity was evaluated in vivo. Among the synthesized compounds, C8 phenyl-substituted AHX showed remarkable growth-promoting activity on rice. The present study shows the power and significant opportunity of C–H functionalization chemistry to rapidly transform biologically active natural products into more active compounds.