The invention discloses a 2-(2-iodoaryl)quinazoline compound and a preparation method thereof. The 2-(2-iodoaryl)quinazoline compound is prepared by using 2-arylquinazoline as a reaction substrate through the process of carbon-hydrogen bond activation iodination with iodosuccinimide under the catalytic action of dichloro(pentamethylcyclopetadienyl)rhodium (III) dimer/silver hexafluoroantimonate, wherein the reaction temperature is 85 DEG C, and the reaction time is 1 to 2 hours. The preparation method provided by the invention has the advantages of high yield, excellent reaction chemical selectivity, mild reaction conditions, simple and convenient operation, low cost, less side reaction and high product purity; and the product disclosed by the invention is a novel compound, facilitates to separation and purification, is applicable to large-scale preparation, and has good application value and potential biological activity.