| 摘要 |
PROBLEM TO BE SOLVED: To obtain the subject new production intermediate enabling the industrial production of a pyrimidine derivative useful as pharmaceuticals, agrochemicals, etc., by reacting a specific pyrimidine derivative with carbon disulfide and an alkylation agent. SOLUTION: The objective compound of formula I (R<1> is H, a halogen or OH; R<2> is a 1-4C alkyl.) [e.g. (±)-5-chloro-6-(1-fluoroethyl)-4-[2-(4-(methylthio thiocarbonyloxy)phenyl)ethy]aminolpyrimidine] is produced by reacting a 4-[2-(4- hydroxyphenyl)ethylaminolpyrimidine derivative of formula II with carbon disulfide and an alkylation agent expressed by the formula R<2> -X (X is a halogen or a sulfuric acid ester residue) (e.g. methyl iodide). Preferably, the compound of formula I is made to react with hydrogen fluoride.pyridine in the presence of 1,3-dibromo-5,5-dimethylhydantoin to obtain a 4-[2-(4-(trifluoromethoxy) phenyl) ethylamino]pyrimidine derivative of formula III.
|
