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Updated: Mar 28, 2026

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Published on: July 30, 2017
Palladium-Catalyzed C-H Arylation of Indoles at the C7 Position
Youqing Yang1, Xiaodong Qiu1, Yue Zhao1
1State Key Laboratory of Coordination Chemistry, Collaborative Innovation Center of Chemistry for Life Sciences, School of Chemistry and Chemical Engineering, Nanjing University , Nanjing 210093, China.
Abstract:
In the past decade, direct C-H arylation of indoles has been developed with high selectivity at the C2 and C3 positions via transition-metal-catalyzed cross-coupling reactions. Here we show that C-H activation can be directed to the C7 position with high selectivity in Pd-catalyzed coupling of indoles with arylboronic acids. The key to this high regioselectivity is the appropriate choice of a phosphinoyl directing group and a pyridine-type ligand in the presence of Pd(OAc)2 catalyst. This previously elusive transformation should provide insight for the design of other cross-couplings as well.
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