富马酸替诺福韦二吡呋酯的合成  

Synthesis of Tenofovir Disoproxil Fumarate

作　　者：严楠[1,2] 林春花[1] 熊云奎[1] 夏剑辉[2] 廖维林[2] 

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

出　　处：《精细化工》2014年第8期983-987,共5页Fine Chemicals

基　　金：国家科技支撑计划资助项目(2009BAI75B02);江西省研究生创新基金资助项目(YC2014-B024)~~

摘　　要：该文对以R-碳酸丙烯酯为原料的富马酸替诺福韦二吡呋酯合成工艺进行了改进。改进的反应步骤是采用微波辅助盐酸加快磷酸酯水解,乙醇镁促进烷基化反应,和碘甲基碳酸异丙酯作为有效酯化试剂。改进后的合成工艺总收率从24%提高到33.5%。并且对环境污染较少和总成本较低,适合于工业化生产。In this paper, process improvements of the synthesis of Tenofovir disoproxil fumarate started from （R）-propylene carbonate was optimized. The improved process simply included microwaveassisted acid hydrolysis of phosphonate ester, and alkylation promoted with magnesium ethoxide, with iodine methyl isopropyl carbonate as an efficient esterification reagent. After improvements, not only the overall yield of the synthesis process of Tenofovir disoproxil fumarate was improved from 24% to 33.5% ,but also the identified process was more environmentally friendly, and with lower cost, which was more suitable for robust commercial production.

关 键 词：碘甲基碳酸异丙酯 富马酸替诺福韦二吡呋酯 微波辅助 医药与日化原料 

分 类 号：R977.3[医药卫生—药品]