PURPOSE: To provide a new preparation process of N-[3-(1H-imidazol-1- yl-4-(substd.)-2-pyrimidinamine compound wherein the substituent is 2-pyridinyl, 3-pyridinyl, 4-pyridinyl, 2-furanyl or 2-thienyl.

CONSTITUTION: 3-(1H-Imidazol-1-yl)benzamine is reacted with cyanamide and a halogen acid while controlling the pH of the reaction between about 2 to about 3.5 to form a [3-(1H-imidazol-1-yl)phenyl]guanidine dihydrochloride, reacting the product with an appropriately substd. 3-dimethylamino-1-(substd.)-2- propen-1-one and a base at a pH of about 10.5-11.5 and recovering the N-[3-1H- imidazol-1-yl]phenyl]-4-(substd.)-2-pyrimidinamine compound so produced. The present process can be applied to a compound bearing furyl group and thienyl group at the 4-position, and the desired product is obtained in high yield with high purity.