The Pd‐catalyzed direct arylation of 2,1‐benzisoxazole with aryl bromides to access 3‐arylbenzoisoxazoles proceeds in moderate‐to‐high yields with 1 mol % Pd(OAc)2 or 2 mol % PdCl(C3H5)(dppb) (dppb=1,4‐bis(diphenylphosphino)butane) as the catalysts and KOAc as an inexpensive base. A wide variety of (hetero)aryl bromides have been employed successfully. Moreover, arylations followed by benzisoxazole ring opening allowed the preparation of 2‐aminobenzophenones in only two steps.
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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