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A palladium‐catalyzed, late‐stage functionalization of 4‐alkyl‐1,5‐diaryl‐1 H‐pyrazole‐3‐carboxylates to achieve acetoxylation or iodination via Csp2−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.
Asian Journal of Organic Chemistry – Wiley
Published: Apr 1, 2016
Keywords: ; ; ; ;
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