论文部分内容阅读
Heterocycles such as 2-oxindoles and benzo-1,3-diazoles have become the privileged scaffolds for pharmaceutical design and drug discovery and hold a special place among pharmaceutically significant natural products and synthetic compounds.[1] Furthermore,the often at the C-3 substituted of 2-oxindoles and C-2 position substituted of benzo-1,3-diazoles can effectively enhance the biological activity of these compounds.On the other hand,two pharmacophoric groups covalently bounded via a linkage are expected to elicit increased pharmacological action or dual efficacy.[2] Therefore,it is highly prospective to develop the facile and efficient method for gem-difluoromethylene moiety linked diheterocyclic compounds through benzo-1,3-azolic(oxa-or thia-)difluoromethyl radicals generated by Cu(I)single electron transformation was added to terminal of C-C double bond of N-arylacrylamides,followed by cyclization to 2-oxindoles under mild conditions(Scheme 1).