The application relates to an indole derivative obtained by converting
quinoline nitrogen-
oxide and a synthesis method of the indole derivative, the chemical
structural formula of the derivative is shown as formula 2; the synthesis method is as follows:
quinoline nitrogen-
oxide, dimethyl
acetylene dicarboxylate and water are used as reaction raw materials and are added into 1,2-
dichloroethane solvent, a first heating stirring reaction is carried out under the
catalysis of
diphenyl phosphate, after TLC monitoring shows that the conversion of
quinoline nitrogen-
oxide of formula 1 compound is complete,
trichloroacetic acid and
molecular sieve dehydrating agent are added, a second heating stirring reaction is carried out, the reaction is monitored until complete through TLC, the
solvent is evaporated, and then purification is carried out to obtain the indole derivative. The method has the advantages of high
atom economy, mild reaction condition, green, low cost, high conversion rate and the like, meanwhile, the method is a carbon recombination strategy for directly editing a molecular skeleton, can provide a new idea for late-stage design and optimization of a
drug molecule, and can accelerate the
drug discovery and development process, and has good theoretical value and application prospect.