替诺福韦艾拉酚胺的合成

摘要

We initially designed a route to synthesize of tenofovir alafenolide,where using R-propylene oxide and adenine as starting materials to obtain R-9-(2-hydroxypropyl)adenine(HPA),then reacted with p-toluenesulfonyl oxymethyl benzyl phenyl phosphonate and alanine isopropyl ester successively to get tenofovir alafenamide(TAF).This method used inexpensive R-propylene oxide instead of the expensive R-propylene carbonate to make the process cheaper and simpler.%初步总结设计了一条替诺福韦艾拉酚胺的合成工艺路线,以R-环氧丙烷与腺嘌呤为起始原料,得到R-9-(2-羟基丙基)腺嘌呤(HPA),再经与对甲苯磺酰氧甲基苄基苯基膦酸酯、丙氨酸异丙酯反应得到替诺福韦艾拉酚胺(TAF).该方法采用廉价的R-环氧丙烷替代价格昂贵的R-碳酸丙烯酯,使得工艺更为廉价、简洁.