富马酸替诺福韦二吡呋酯的合成

Synthesis of Tenofovir Disoproxil Fumarate

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，适合于工业化大生产

Abstract:

In this paper, process improvements of the synthesis of Tenofovir disoproxil fumarate started from (R)-propylene carbonate was optimized. The process improvements were included in simply microwave-assisted acid hydrolysis of phosphonate ester, alkylation promoted with magnesium ethoxide, and iodine methyl isopropyl carbonate as an efficiently esterification reagent. The overall yield of the process of synthesis of Tenofovir disoproxil fumarate was not only improved from 24% to 33.5%, but also the identified process were more environmentally friendly, lower cost, and more suitable for productive and robust production.