Pd‐Catalyzed Late‐Stage Monoacetoxylation and Monoiodination of 4‐Alkyl‐1,5‐diaryl‐1 H‐pyrazole‐3‐carboxylates via Direct Csp2−H Bond Activation

A palladium-catalyzed, late-stage functionalization of 4-alkyl-1,5-diaryl-1H-pyrazole-3-carboxylates to achieve acetoxylation or iodination via Csp(2)-H bond activation with synthetically useful to excellent yields is described. These straightforward transformations feature highly functionalized substrates, excellent site selectivity, rapid reaction, and simple operation. The C-O and C-I bond-forming protocols allow convenient accesses to lots of complex monoacetoxylated and monoiodinated products from pharmaceutically important intermediates. Iodoacetic acid is also used as the iodinating agent in C-H bond activation.