The palladium‐catalyzed direct arylation of 2 H‐indazoles with aryl bromides for the preparation of 3‐aryl‐2 H‐indazoles was found to proceed in high yields when using only 0.5–0.1 mol % Pd(OAc)2 catalyst and KOAc as… Click to show full abstract
The palladium‐catalyzed direct arylation of 2 H‐indazoles with aryl bromides for the preparation of 3‐aryl‐2 H‐indazoles was found to proceed in high yields when using only 0.5–0.1 mol % Pd(OAc)2 catalyst and KOAc as inexpensive base. A wide variety of electron‐deficient and electron‐rich aryl bromides and also heteroaryl bromides has been successfully employed. Both electron‐withdrawing and electron‐donating substituents on the 2 H‐indazoles are also tolerated. Moreover, the reaction can be performed in the “green” solvent cyclopentyl methyl ether.
               
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