Reactivity of 2,1‐Benzisoxazole in Palladium‐Catalyzed Direct Arylation with Aryl Bromides

Abstract 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(C 3 H 5 )(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.