A novel synthesis of 2-aryl-2H-indazoles via a palladium-catalyzed intramolecular amination reaction |
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| Authors: | Song J J Yee N K |
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| Institution: | Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut 06877-0368, USA. jsong@rdg.boehringer-ingelheim.com |
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| Abstract: | reaction: see text] A variety of 2-aryl-2H-indazoles were synthesized by the palladium-catalyzed intramolecular amination of the corresponding N-aryl-N(o-bromobenzyl)hydrazines. Of several sets of reaction conditions surveyed, the combination of Pd(OAc)2/dppf/tBuONa gave the best results. This method applies to a wide scope of substrates containing electron-donating and electron-withdrawing substituents. |
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