地西他滨的合成  

Synthesis of Decitabine

作　　者：季竞竞[1] 杨守宁[1] 董冬吟[1] 杨琍苹[1] 

机构地区：[1]华东师范大学化学系,上海200062

出　　处：《中国医药工业杂志》2007年第7期468-469,共2页Chinese Journal of Pharmaceuticals

摘　　要：2-脱氧-D-核糖在吡啶作用下与乙酐进行乙酰化,再在TMSOTf作用下与5-氮杂胞嘧啶偶联得1-(3,5-二-O-乙酰基-2-脱氧-D-核糖)-5-氮杂胞嘧啶,最后经氨气脱保护、甲醇重结晶得抗肿瘤药地西他滨,总收率约32%。Decitabine was synthesized from 2-deoxyribose by acetylization with acetic anhydride, coupling with 5-azacytosine catalyzed by TMSOTf to get 1-（3,5-di-O-acetyl-2-deoxy-D-ribofuranosyl）-5-azacytosine, followed by deprotection and recrystallization with an overall yield of about 32 %.

关 键 词：地西他滨 抗肿瘤药 骨髓增生异常综合征 合成 

分 类 号：R979.1[医药卫生—药品]