Xu Hui, Fan Ling-Ling
Laboratory of Pharmaceutical Synthesis, College of Sciences, Northwest A&F University, Yangling 712100, China.
Chem Pharm Bull (Tokyo). 2009 Mar;57(3):321-3. doi: 10.1248/cpb.57.321.
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.
已开发出一种高效的一锅逐步叔丁醇钾介导的合成N-芳基吲哚的方法，产率适中至良好。该方案包括将N-芳基磺酰基吲哚作为潜在吲哚进行连续脱保护，以及随后与活性芳基卤化物进行S(N)Ar反应。这种串联反应提供了一种高效且方便的制备N-芳基吲哚的方法，该方法受益于芳基磺酰基对吲哚的预先保护，并且可以缩短反应序列并提高合成效率。
