| Due to dramatic drug activity and unique structural framework,indole dereivatives was widely used in the pharmaceutical industry and the synthesis of natural products.In recent studies,other group developed a valuable method of the direct allylation of indoles with different halogen contents that are allyl halides,allyl acetates and allyl carbonates.However,because of existing multiple reaction sites of indole,most of procedures generally suffered from poor selectivity problems associated with the regiochemistry of alkylation.And this kind of reaction had the characteristics of lower yield,longer reaction time and functional intolerance with expensive catalysts.In order to changing the situitions,it is valuable task that novel methods and catalysts which involved efficient,inexpensive and environmentally for the allylation of indoles with higher yield was explored.In this paper,we studied that the regioselective C-2 allylation of indoles has also been achieved with using C-2-alkylated indole and allyl halides.C-2allylation of indoles and its derivatives can be transmitted by C-2-substituded indole,allyl halide and Cu?OTf?2.We tried our best to study the most optimal conditions of the reaction and explore the universality of substrate.In addition,we proposed the possible mechanism of the reaction by catching the free radical.We have developed a simple procedure for the clean regioselective C-2-allylation by a catalytic system Cu???of inexpensive and environmentally.The other advantages of this procedure included shorter reaction time and excellent regioselectivity with higher yield.This was valuable method of synthesizing allylation of indoles.In this process of allylation reaction of indoles,we also found thatallyl alcohol can constitute ketone without metal catalyst.Though the long term researching,it can be concluded that allyl alcohol can be oxidized to ketone under the condition of DUB catalytic with high yield and good substrate universality. |
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