A process for the preparation of nucleosides, derivatives and analogues thereof by coupling reaction of a protected suitable nitrogeneous purine or pyrimidine base, a derivative or analogue thereof and a protected suitable sugar in the presence of SnCl
4
comprising the removal of SnCl4 by adding DMSO directly into the reaction mixture is described. Preferably said process is used for the preparation of antiviral and antitumor agents having a nucleoside or nucleoside-like structure, still more preferably for the preparation of azacytidine, decitabine, chlorfarabine, cladribine, mizoribine. A residual tin content lower than 300 ppm is obtained with said process.
一种通过在SnCl4存在下,将受保护的适当氮碱基与其衍
生物或类似物以及受保护的适当糖进行偶联反应来制备核苷、其衍
生物和类似物的方法,其中通过向反应混合物中直接加入
DMSO来去除SnCl4。该方法通常用于制备具有核苷或类似核苷结构的抗病毒和
抗肿瘤药物,更喜欢用于制备氮杂
胞苷、
地西他滨、
氯法比林、克拉德比林、米佐利宾。使用该方法可以获得低于300 ppm的残留
锡含量。