Microwave-assisted solid-phase organic synthesis (MASPOS) as a key step for an indole library construction

被引：70
作者：
Dai, WM [1 ]
Guo, DS
Sun, LP
Huang, XH
机构：
[1] Hong Kong Univ Sci & Technol, Biotechnol Res Inst, Combinatorial Chem Lab, Kowloon, Hong Kong, Peoples R China
[2] Hong Kong Univ Sci & Technol, Dept Chem, Kowloon, Hong Kong, Peoples R China
来源：
ORGANIC LETTERS | 2003年 / 5卷 / 16期
关键词：
D O I：
10.1021/ol0350543
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
graphics 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 degreesC [for Cu(OAc)(2), NMP] or 160 degreesC [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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页码：2919 / 2922
页数：4
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