富马酸替诺福韦二吡呋酯的合成

Synthesis of Tenofovir disoproxil fumarate

实验以(R)-(+)-9-(2-羟丙基)腺嘌呤为起始原料,经膦酸酯缩合反应、水解反应、取代反应、成盐反应及重结晶提纯5个步骤而得到富马酸替诺福韦二吡呋酯成品,总收率51.0%。目标产物结构经^(1)H NMR、^(13)C NMR、HI-MS表征。该工艺路线用到的试剂常见,各步反应条件温和,后处理操作简易,适合工业化生产。

Tenofovir disoproxil fumarate was prepared via phosphonate condensation,hydrolysis,substitution,salt formation and recrystallization reaction using(R)-(+)-9-(2-hydroxypropyl)adenine as raw material.The total yield of the product can be up to 51.0%.The structures of the target compound were confirmed by^(1)H NMR,^(13)C NMR and HI-MS.The reagents used in this technical process route are common,the reaction conditions of each step are mild,the post-treatment operation is simple,so it is suitable for industrial production.