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期刊论文

Microwave-Assisted Solid-Phase Organic Synthesis (MASPOS) as a Key Step for an Indole Library Construction†

戴伟民Wei-Min Dai* Dian-Shun Guo Li-Ping Sun and Xiang-Hong Huang

Org. Lett., Vol. 5, No.16, 2003,-0001,():

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摘要/描述

Microwave-assisted solid-phase organic synthesis (MASPOS) has been demonstrated to significantly facilitate the Cu(II)-or Pd(II)-mediated ring closure of the resin-bound 2-alkynylanilides. Under microwave irradiation at 200℃ [for Cu(OAc)2, NMP] or 160℃ [for Pd(MeCN)2Cl2, THF] for 10min, 1-acyl-2-alkyl-5-arenesulfamoylindoles were obtained, after cleavage from the resin, in 95-99% purities and in 65-82% overall yields via a 5-step synthetic sequence.

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