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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
Author(s) -
Belkessam Fatma,
Aidene Mohand,
Soulé JeanFrançois,
Doucet Henri
Publication year - 2017
Publication title -
chemcatchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.497
H-Index - 106
eISSN - 1867-3899
pISSN - 1867-3880
DOI - 10.1002/cctc.201601420
Subject(s) - aryl , indazole , palladium , catalysis , chemistry , phosphine , medicinal chemistry , solvent , ether , base (topology) , organic chemistry , alkyl , mathematics , mathematical analysis
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.