【摘要】 (R)-1,2-丙二醇与碳酸二乙酯经缩合、与腺嘌呤反应、与对甲苯磺酰氧甲基硫代膦酸二乙酯缩合、水解、保护氨基后氯代制得(R)-9-[2-(二氯硫代膦酰基甲氧基)丙基]腺嘌呤,与(S)-(-)-(3-氯苯基)-1,3-丙二醇在四氯化钛作用下反应后再经富马酸成盐制得抗病毒药富马酸替硫福韦酯,总收率约13%(以(R)-1,2-丙二醇计)。更多还原

【Abstract】 Tesuofovir circularproxil fumarate was synthesized from from(R)-1,2-propanediol by condensation,reaction with adenine,condensation,hydrolysis,protection and chlorination to give(R)-9-[2-(dichlorothiophosphorylmethoxy)propyl]adenine,which was subjected to reaction with(S)-(-)-(3-chlorophenyl)-1,3-propanediol in the presence of TiCl4 and then salification with an overall yield of about 13%(based on(R)-1,2-propanediol).更多还原