卡培他滨中间体5'-脱氧-5-氟胞苷的合成新方法

Synthesis of Capecitabine Intermediate 5'-Deoxy-5-fluorocytidine

以5-氟胞苷为原料,在PPh3/Br2作用下,选择性地在5'羟基发生溴代反应,继而用Pd/C将溴原子还原脱除,以两步反应和52%的总收率得到标题化合物。该方法原料易得,路线简单,收率高,产物构型单一,为卡培他滨及该类化合物的合成提供了新的途径,具有潜在的应用前景。

The capecitabine intermediate 5 ＇-deoxy-5-fluorocyt- idine was synthesized from 5-fluorocytidine via selective bro- mination by PPh3/Br2 at 5＇ position and hydrogenation by Pd/ C within two steps and 52% yield. This method takes advan- tages of availab]e materials, short reaction steps, pure configu- ration and excellent yield, providing new avenue of synthesi- zing 5＇-deoxy-5-fluorocytidine and its derivatives, indicating potential application prospect.