申请人:Daikin Kogyo Co., Ltd.
公开号:EP0111299A1
公开(公告)日:1984-06-20
A fluorine-containing uridine derivative of the formula:
wherein R is lower acyl, fluorine-containing lower acyl or fluorine-containing lower alkyl; and X is hydrogen or hydroxyl, which is prepared by a process fluorinating 2', 3'-O-isopropylideneuridine with fluorine in a solvent selected from the group consisting of lower carboxylic acids, fluorine-containing lower carboxylic acids and fluorine-containing lower alcohols, and is converted to a 5-fluorouridine derivative of the formula:
wherein R and X are as defined above by reacting the fluorine-containing uridine derivative of the formula (I) with a base in an organic solvent at a temperature of 0 to 80°C.
式中 R 为低级酰基、含氟低级酰基或含氟低级烷基;X 为氢或羟基的含氟尿苷衍生物,其制备方法是在选自低级羧酸、含氟低级羧酸和含氟低级醇的溶剂中将 2',3'-O-异亚丙基尿苷与氟氟化,并在 0 至 80°C 温度下在有机溶剂中将式(I)的含氟尿苷衍生物与碱反应,转化为式中 R 和 X 如上定义的 5-氟尿苷衍生物。