The invention relates to chiral 2,3-dihydropyrrole[1,2-a] indole derivatives with a
biological activity and an asymmetric synthesizing method thereof. The derivatives have a structure of a general formula I, in which R1 is
hydrogen, 6-methyl, 7-methyl, 8-methyl, 7-methoxyl, 6-
fluorine, 6-
chlorine, 7-
fluorine, 7-
chlorine, 7-
bromine or 7-benzyloxyl; R2 is methyl, ethyl,
isopropyl, cyclohexyl, phenyl, benzyl, dimethyl
tertiary butyl siloxy ethyl, benzosuccinimide ethyl or CH2CO2Me; R3 is phenyl, 4-methyl phenyl, 4-methoxyl phenyl, 4-fluorophenyl, 4-chlorphenyl, 4-bromophenyl, 3-bromophenyl, 2-fluorophenyl, 2-thienyl, styryl, ester group or cyclohexyl; and R4 is methyl, ethyl,
isopropyl or benzyl. The derivatives are synthesized by Michael-semiacetalation
cascade reaction of 3-substituted indole and beta, gamma-unsaturated alpah-keto ester catalyzed by
copper trifluoromethanesulfonate and
oxazoline ligand.