| 摘要 |
PURPOSE:To obtain the subject derivative useful as pharmaceuticals, agricultural chemicals, etc., using a short synthesis route in high operability and yield by cross-coupling a Grignard reagent of a halogenophenylpyridine with a halogenopyrimidine derivative in the presence of a palladium catalyst, etc. CONSTITUTION:The objective derivative of formula V can be produced by cross-coupling a substituted phenylboric acid of formula I (R<1> and R<2> are H, F, trifluoromethyl, trifluoromethoxy, alkyl or alkoxy) with a 2,5- dihalogenopyridine of formula II (X is Cl or Br) in the presence of a base and a palladium catalyst, converting the obtained 5-halogeno-2-phenylpyrimidine derivative of formula III to the corresponding Grignard reagent and cross- coupling the Grignard reagent with a 2-halogenopyrimidine derivative of formula IV (R<3> is H, F, trifluoromethyl, etc.; Y is Cl or Br) in the presence of a palladium or nickel catalyst. |
