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Direct C3‐Arylation of 2 H‐Indazole Derivatives with Aryl Bromides by using Low Loading of a Phosphine‐free Palladium Catalyst

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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.

Keywords: direct arylation; aryl bromides; electron; palladium; catalyst

Journal Title: ChemCatChem
Year Published: 2017

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