title: Microwave-assisted solid-phase organic synthesis (MASPOS) as a key step for an indole library construction.
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.
authors.affiliation: 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
authors.forename: Wei-Min
authors.initials: WM
authors.lastname: Dai
authors.forename: Dian-Shun
authors.initials: DS
authors.lastname: Guo
authors.forename: Li-Ping
authors.initials: LP
authors.lastname: Sun
authors.forename: Xiang-Hong
authors.initials: XH
authors.lastname: Huang