The invention discloses a method for preparing a naphthodiazepine indole derivative, which comprises the following steps: adding tri (
dibenzylideneacetone) dipalladium (0)-
chloroform adduct, bis (2-diphenylphosphinophenyl)
ether and alkali into a reactor, adding a certain amount of
solvent under the protection of
argon, and stirring for a period of time; the preparation method comprises the following steps: dissolving N-(4-methylbenzenesulfonyl)-1-(2-indolyl)-2-
naphthylamine and methyl (1-arylpropyl-2-
alkyne-1-yl)
carbonate in a certain amount of
solvent, adding into a reactor, reacting at
room temperature, and detecting that the reaction is complete by TLC (
Thin Layer Chromatography). And after the reaction is finished, filtering, concentrating filtrate under reduced pressure, and performing
column chromatography to obtain a pure product of the naphthodiazepine indole derivative. According to the technical scheme, the method has the characteristics of diversified substrate
raw material sources, simple synthesis steps, mild
reaction conditions, simplicity and convenience in operation, good reaction selectivity, complex and diversified target compound structures, and the like, and the product further contains olefin and amino functional groups for further structural modification.