Microwave-assisted solid-phase organic synthesis (MASPOS) as a key step for an indole library construction |
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| Authors: | Dai Wei-Min Guo Dian-Shun Sun Li-Ping Huang Xiang-Hong |
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| Institution: | Combinatorial Chemistry Laboratory, The Biotechnology Research Institute and Department of Chemistry, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong SAR, China. chdai@ust.hk |
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| Abstract: | reaction: see text] 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 degrees C for Cu(OAc)(2), NMP] or 160 degrees C for Pd(MeCN)(2)Cl(2), THF] for 10 min, 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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