Herein, a one-pot protocol for constructing the disubstituted isoquinolinone derivatives via the three-component reactions of 3-haloisoquinolines, alkyl halides, and indoles under transition-metal-free conditions is described. The reaction realized the trifunctionalization of isoquinoline via a dearomatization strategy, which displayed high chemical selectivity, excellent functional group tolerance, and a wide range of substrates, and is environmentally friendly. The three-component coupling involves the construction of new C−N, C�O, and C−C bonds in one step.
The efficient three‐component cascade coupling reaction of 3‐haloisoquinolines, haloalkanes, and sp3‐carbon nucleophiles (acetophenone or nitromethane) led to a series of structurally novel 1,2‐disubstituted‐3‐isoquinolinones through the formation of C(sp3)−C(sp2), C−N, and C=O bonds. The NaOAc‐promoted reaction described in this work is simple to operate, environment friendly, and highly selective.
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