5-甲基尿苷的合成  

Synthesis of 5-Methyluridine

作　　者：吴嘉圣 

机构地区：[1]上虞盛晖化工有限公司,浙江上虞312369

出　　处：《浙江化工》2013年第3期17-19,共3页Zhejiang Chemical Industry

摘　　要：胸腺嘧啶与六甲基二硅胺烷反应生成双三甲硅基胸腺嘧啶,再和四乙酰核糖缩合反应后经醇解反应制备5-甲基尿苷。对缩合反应路易斯酸催化剂三氯化铝、四氯化锡和氯化锌进行了比较,实验结果表明:催化效果:四氯化锡(产率85%)>氯化锌(产率82%)>三氯化铝(产率10%),但氯化锌具备价格优势;对醇解反应碱催化剂氨、甲醇钠进行了比较,实验结果表明催化用氨和甲醇钠最终产率接近,催化速度:甲醇钠>氨。Bis-trimethylsilyl-thymine was synthesized by thymine and hexamethyl disilylamine.Then,using 1,2,3,5-tetra-O-acetyl-D-ribose condensation-reacted with bis–trimethylsilyl-thymine,alcoholysis-reacted with methanol to prepared 5-methyluridine.In condensation reaction,the Lewis acid catalyst of aluminum trichloride,tin tetrachloride and zinc chloride were compared,the experimental results show that the catalytic effect of tin tetrachloride（yield：85%） zinc chloride（yield： 82%） three aluminum chloride（yield：10%）,but zinc chloride have the price advantage.In alcoholysis,base catalyst of ammonia,sodium methoxide were compared,the experimental results show that close to the ultimate yield of the catalytic with ammonia and sodium methoxide,the rate of catalysis of sodium methoxide ammonia.

关 键 词：胸腺嘧啶 四乙酰核糖 5-甲基尿苷 抗艾滋病药物 

分 类 号：TQ463[化学工程—制药化工]