One-pot N-arylation of indoles directly from N-arylsulfonylindoles via consecutive deprotection and S(N)Ar Reactions with activated Aryl halides.
An efficient one-pot step by step t-BuOK-mediated procedure for the synthesis of N-arylindoles has been developed in moderate to good yields. The protocol involves the consecutive deprotection of N-arylsulfonylindoles as latent indoles and subsequent S(N)Ar reactions with activated aryl halides. This tandem reaction affords an efficient and convenient preparation of N-arylindoles that benefit from prior indoles protection by arylsulfonyl group, and can shorten a reaction sequence and improve synthetic efficiency.
Xu
Hui
H
Laboratory of Pharmaceutical Synthesis, College of Sciences, Northwest A&F University, Yangling 712100, China. orgxuhui@nwsuaf.edu.cn
Fan
Ling-Ling
LL
D001128:Argon / Q000737:chemistry*; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry; D009584:Nitrogen / Q000737:chemistry*; D013455:Sulfur / Q000737:chemistry*; D013997:Time Factors
D007211:Indoles; D001128:Argon; D013455:Sulfur; D009584:Nitrogen