The accelerated development of an optimized synthesis of 1,2,4-oxadiazoles: application of microwave irradiation and statistical design of experiments

被引:67
作者
Evans, MD
Ring, J
Schoen, A
Bell, A
Edwards, P
Berthelot, D
Nicewonger, R
Baldino, CM
机构
[1] ArQule Inc, Dept Chem, Woburn, MA 01801 USA
[2] Pfizer Ltd, Global Res & Dev, Lib Design & Prod Grp, Sandwich Labs, Sandwich CT13 9NJ, Kent, England
关键词
oxadiazole; microwave; design of experiments; amidoxime; optimization;
D O I
10.1016/j.tetlet.2003.10.055
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Herein, we report the development of an optimized microwave-assisted synthesis of 1,2,4-oxadiazoles. The chemistry development process was significantly accelerated by employing a statistical software package (MODDE 6.0(TM)) to guide in the optimization of the reaction conditions. The resulting optimized reaction conditions were then utilized in the synthesis of a focused library of 1,2,4-oxadiazoles. (C) 2003 Published by Elsevier Ltd.
引用
收藏
页码:9337 / 9341
页数:5
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