Direct C‐3‐Arylations of 1 H ‐Indazoles

Direct C‐3‐Arylations of 1 H ‐Indazoles

The first example of intermolecular C–H arylation of substituted 1 H ‐indazoles is reported. Various 1‐substituted indazoles were used as starting materials, and (hetero)aryl bromides and iodides were investigated as coupling partners. Different reaction conditions were investigated. The best result...

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Bibliographic Details
Published in:European journal of organic chemistry Vol. 2012; no. 36; pp. 7075 - 7081
Main Authors: Ben‐Yahia, Ali, Naas, Mohammed, El Kazzouli, Saïd, Essassi, El Mokhtar, Guillaumet, Gérald
Format: Journal Article
Language:English
Published: 01-12-2012
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Summary:The first example of intermolecular C–H arylation of substituted 1 H ‐indazoles is reported. Various 1‐substituted indazoles were used as starting materials, and (hetero)aryl bromides and iodides were investigated as coupling partners. Different reaction conditions were investigated. The best results were obtained using Pd(OAc) 2 as catalyst, 1,10‐phenanthroline as ligand, K 2 CO 3 as base, and DMA as solvent. The crucial role of the ligand on the C–H arylation of substituted 1 H ‐indazoles is highlighted.
ISSN:1434-193X
1099-0690
DOI:10.1002/ejoc.201200860