摘要 |
PURPOSE:Readily available 5-fluoro-6-halouracil is used as a starting material to give the titled compound used as an antitumor agent only by reduction through simple and safe process. CONSTITUTION:For example, a fluorobarbituric acid derivative is allowed to react with a halogenation agent such as phosphorus oxychloride to readily give 5-fluoro-6-halouracil derivative of furmula I (X is Cl, B, I; R<1>, R<2> are H, alkyl, aralkyo, aryl or oxygen-containing heterocyclic ring) such as 5-fluoro-6-chlorouracil. Then the product is reduced with hydrogen in the presence of a transition metal catalyst and a base to give 5-fluorouracil derivative of formula II such as 5-fluorouracil. |