The invention discloses a method for synthesizing chlorambucil, which relates to the technical field of organic chemistry, and comprises the following steps: S1, adding a mixture of 4-bromo-N, N-bis (2-chloroethyl) aniline, N-(quinolin-8-yl) butyl 3-enamide, palladium chloride, tri-n-butylphosphine tetrafluoroborate, potassium carbonate and benzoic acid at ratio of 10.83%: 10.83%-32.50%: 0.22%-2.17%: 0.43%-2.17%: 10.83%-54.17%: 10.83%-54.17% and dimethyl sulfoxide at molar volume ratio of 0.1 mmol: 2 mL to a reaction vessel for uniform mixing; and S2, placing the reaction container in an oil bath at 135-145 DEG C, and violently stirring to react for 24 hours. According to the invention, through the coupling reaction, 8-aminoquinoline is designed as a compound of a leaving group to control regioselectivity and chemical selectivity in the reaction, so that the problem of excessive steps in the existing synthesis process of chlorambucil is effectively solved; the method has the characteristics of high reaction region selectivity and yield, mild reaction conditions and simple reaction and post-treatment purification processes.