| 摘要 |
PURPOSE: To easily obtain the subject compound useful as a synthetic intermediate for carcinostatic agent and antiviral agent from inexpensive raw materials in high yield by trifluoromethylating a halogenated uracil derivative having a specific structure. CONSTITUTION: The objective compound of formula II is produced by trifluoromethylating a 5-halogenated uracil derivative of formula I (R<1> and R<2> are each H, a 1-10C alkyl, benzyl, etc.; X is Cl, I or Br) with preferably 0.5-5 times mol (based on the compound of formula I) of 2,2- difluoro-2-(fluorosulfonyl)acetic acid methyl ester. Preferably, copper or copper iodide is used as a catalyst and DMF is used as a reaction solvent in the above reaction. The reaction is carried out at 50-150 deg.C for 3-10hr. N<1> ,N<3> -dibenzyl-5- trifluoromethyluracil of formula III is a new compound among the compounds of formula II. The compound of formula III can be produced e.g. from N<1> ,N<3> - dibenzyl-5-iodouracil. |
