阿扎胞苷的合成工艺研究

Synthetic process of azacitidine

目的研究阿扎胞苷的合成工艺。方法以5-氮杂胞嘧啶为原料,在硫酸铵的催化下用双三甲基二硅胺(HMDS)保护其羰基和氨基,再与四乙酰核糖缩合,在甲醇中进行醇解,吡啶重结晶得阿扎胞苷。结果本工艺的总收率为58.8%。结论该合成工艺反应条件温和,操作简便,阿扎胞苷产品质量分数和收率较高,适合于工业化生产。

Objective To study the synthetic process of azacitidine. Methods Using 5-azacytosine as starting materials, In catalytic of ammonium sulfate, carbonyl and amino were protected with HMDS, and combined with tetraacetylribose, azacitidine was obtained by alcoholysis in methanol and recrystallization with pyridine. Results The total yield is 58.8%. Conclusion The technology is stable, simple, high productive, and can be applied to industry of azacitidine.