目的 研究阿扎胞苷的合成工藝。方法 以5-氮雜胞嘧啶為原料，在硫酸銨的催化下用雙三甲基二硅胺（HMDS）保護其羰基和氨基，再與四乙酰核糖縮合，在甲醇中進行醇解，吡啶重結(jié)晶得阿扎胞苷。結(jié)果 本工藝的總收率為58.8%。結(jié)論 該合成工藝反應(yīng)條件溫和，操作簡便，阿扎胞苷產(chǎn)品質(zhì)量分數(shù)和收率較高，適合于工業(yè)化生產(chǎn)。

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.