The invention relates to an indole derivative obtained by converting
quinoline nitrogen-
oxide and a synthesis method thereof. The chemical
structural formula of the derivative is as shown in formula 2. The synthesis method comprises the following steps: adding a compound
quinoline nitrogen-
oxide as shown in a formula 1, dimethyl butynedioate and water serving as reaction raw materials into a 1, 2-
dichloroethane solvent, carrying out a first heating and stirring reaction under the catalytic action of
diphenyl phosphate, and after TLC monitors that the compound
quinoline nitrogen-
oxide as shown in the formula 1 is completely converted, carrying out a second heating and stirring reaction; and adding
trichloroacetic acid and a dehydrating agent # imgabs0 #
molecular sieve, carrying out a second heating and stirring reaction, monitoring the reaction by TLC until the reaction is complete, evaporating out the
solvent, and purifying to obtain the product. The method has the advantages of being high in
atom economy, mild in reaction condition, green, low in cost, high in conversion rate and the like, meanwhile, the method is a carbon recombination strategy for directly editing a molecular skeleton, and a new thought can be provided for later design optimization of
drug molecules. The method can accelerate the
drug discovery and development process, and has good theoretical value and application prospect. # imgabs1 #