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Syntheses of aromatic substituted 6'-thiothalidomides.

  作者 Luo, Weiming;Yu, Qian-sheng;Tweedie, David;Deschamps, Jeffery;Parrish, Damon;Holloway, Harold W.;Li, Yazhou;Brossi, Arnold;Greig, Nigel H.;  
  选自 期刊  Synthesis;  卷期  2008年-21;  页码  3415-3422  
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[摘要]A resurgence of interest in thalidomide has occurred as a consequence of its diverse immunomodulatory and anticancer actions, which has fueled interest in synthetic analogs with higher potencies or less undesirable side effect profiles. Several novel arom. substituted 6'-thiothalidomides were synthesized whose synthetic route and strategy were developed on the basis of an anal. of reaction mechanisms. The regioselectivity of mono-thionation of arom. substituted thalidomides with Lawesson's reagent is described, and the chemoselectivity of hydrogenation between the nitro group and the 6'-thiocarbonyl group is discussed.

 
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