The invention relates to the technical field of
chemical synthesis, in particular to a preparation method of a key intermediate of trifluorobenzene
pyrimidine. The key intermediate is N-(5-pyrimidinylmethyl)-2-aminopyridine, and the preparation method comprises the following steps: mixing 2-fluoropyridine and
ammonia water, heating to react, after the reaction is finished, naturally cooling to
room temperature, and slowly releasing residual
ammonia gas in a reaction container; and adding
acetonitrile and 5-bromomethyl
pyrimidine, heating, stirring to react, cooling to normal temperature, keeping the temperature to react for 1 hour, cooling to-5 DEG C, stirring for 2 hours, filtering and
drying to obtain the N-(5-pyrimidinylmethyl)-2-aminopyridine. The target product is obtained by taking 2-fluoropyridine as a starting
raw material through one-pot substitution, and the
route has the advantages of easily available raw materials, controllable cost, simple and easy operation, easily available raw materials, low cost, mild conditions, mature process, high yield and purity, and is suitable for industrial
mass production.