title: Palladium-Catalyzed C-H Arylation of Indoles at the C7 Position.
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.
authors.affiliation: State Key Laboratory of Coordination Chemistry, Collaborative Innovation Center of Chemistry for Life Sciences, School of Chemistry and Chemical Engineering, Nanjing University , Nanjing 210093, China.
authors.forename: Youqing
authors.initials: Y
authors.lastname: Yang
authors.affiliation: State Key Laboratory of Coordination Chemistry, Collaborative Innovation Center of Chemistry for Life Sciences, School of Chemistry and Chemical Engineering, Nanjing University , Nanjing 210093, China.
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Qiu
authors.affiliation: State Key Laboratory of Coordination Chemistry, Collaborative Innovation Center of Chemistry for Life Sciences, School of Chemistry and Chemical Engineering, Nanjing University , Nanjing 210093, China.
authors.forename: Yue
authors.initials: Y
authors.lastname: Zhao
authors.affiliation: State Key Laboratory of Coordination Chemistry, Collaborative Innovation Center of Chemistry for Life Sciences, School of Chemistry and Chemical Engineering, Nanjing University , Nanjing 210093, China.
authors.forename: Yucheng
authors.initials: Y
authors.lastname: Mu
authors.affiliation: State Key Laboratory of Coordination Chemistry, Collaborative Innovation Center of Chemistry for Life Sciences, School of Chemistry and Chemical Engineering, Nanjing University , Nanjing 210093, China.
authors.forename: Zhuangzhi
authors.initials: Z
authors.lastname: Shi