[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.