韦瑞德合成工艺的优化  

The Process Optimization for the Synthesis of Viread

作　　者：严楠[1,2] 芮培欣[1] 熊斌[1] 刘德永[1] 林春花[1] 廖维林 

机构地区：[1]江西师范大学江西省精细化工重点实验室 [2]国家单糖化学合成工程技术研究中心,江西南昌330027

出　　处：《江西师范大学学报（自然科学版）》2014年第4期331-335,共5页Journal of Jiangxi Normal University(Natural Science Edition)

基　　金：国家科技支撑计划(2009BAI75B02);江西省研究生创新专项基金(YC10A051)资助项目

摘　　要：对韦瑞德合成工艺进行优化.以腺嘌呤为起始原料,将其与R-碳酸丙烯酯缩合反应制得(R)-9-(2-羟基丙基)腺嘌呤,经醚化、超声辅助三甲基氯硅烷脱磷酸酯得到替诺福韦,再经碘甲基碳酸异丙酯酯化、成盐得到最终产物韦瑞德,总收率为31%(以腺嘌呤计算),HPLC纯度达99.5%.该优化合成工艺成本低廉,收率高,步骤短,适合于工业化生产.The method for the synthesis of Viread was studied. The target product was synthesized from adenine via ring-opening condensation with（R）-propylene carbonate,etherification and ultrasonic radiation-assisted hydrolysis to give Tenofovir. Which was subjected to reaction with Iodine methyl isopropyl carbonate,followed by salt formation with an overall yield of about 31% ,the HPLC purity was up to 99. 5% . The optimized synthetic process has the ad-vantages of cheapness,high yield,simple and easy work-up. Which was more suitable for industrialized production.

关 键 词：(R)-9-(2-羟基丙基)腺嘌呤 替诺福韦 合成 韦瑞德 

分 类 号：Q626[生物学—生物物理学]