The invention discloses a preparation method of a tetrahydropyrroloquinoline derivative. The preparation method comprises the following steps: cuprous chloride, aminoalkyne and alkyne are added in a reaction flask, a solvent DMF (dimethyl formamide) is added to the reaction flask, an obtained mixture is subjected to a reaction for 30 min at the temperature of 150 DEG C under microwave irradiation, and a target product is obtained. According to the method, the yield is high, the time is short, the cost is low, a used substrate is not limited by terminal alkyne, good applicability to terminal alkyne and non-terminal alkyne is realized, and the defect of gold catalysis for the reaction is overcome; cell viability tests indicate that part of compounds prepared with the method have inhibitory activity on tumor cell proliferation, so that the method has potential application value in antitumor drug discovery.