One-Pot N-Arylation of Indoles Directly from N-Arylsulfonylindoles via Consecutive Deprotection and SNAr Reactions with Activated Aryl Halides

摘要

An efficient one-pot step by step t-BuOK-mediated procedure for the synthesis of N-arylindoles has been de_veloped in moderate to good yie~1ds. The protocol involves the consecutive deprotection of N-arylsulfonylindoles as latent indoles and subsequent SNAr reactions with activated ary~1 halides. This tandem reaction affords an effi_cient 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.