Hongni Qin, Fan Wu, Yuzhen Xie, Yong Zhang, Song Sun
A visible-light-promoted radical acylmethylation/annulation cascade reaction of N-(2-methylallyl)-2-arylindoles has been accomplished by using sulfoxonium ylides as the acylmethyl sources. Under photoredox catalysis, this method efficiently delivers a series of acylmethylated indolo[2,1-a]isoquinolines in moderate to good yields. Remarkably, the transformation proceeds under mild conditions, is operationally simple, accommodates a broad range of substrates, and exhibits excellent functional group tolerance.