【摘要】 目的:(R)-9-[2-(二乙氧基磷酰甲氧)丙基]腺嘌呤(3)合成过程中的催化剂优选。方法:以亚磷酸二乙酯和多聚甲醛经缩合、酯化得到对甲苯磺酸羟甲基磷酸二乙基酯(1)。另以(R)-1,2-亚丙基碳酸酯与腺嘌呤反应得到9-(2-羟丙基)腺嘌呤(2),在(1)与(2)缩合得到(3)的反应中对四种催化剂进行实验对比。结果:优选催化剂为叔丁醇锂的无水DMF溶液,降低成本和污染。结论:合成得到(3),产率提高到40.5%。更多还原

【Abstract】 Objective:Optimization of the catalyst in the synthetic process of(R)-9-[2- (Diethylphosphonome-oxy)propyl]adenine(3).Methods:Diethyl[[(p-Toluenesulfonyl)oxy]methyl]phosphonate (1) was prepared from diethylphosphate and paraformaldehyde by condensation and esterification.9- (2-hydroxy-propyl)adenine(2) was synthesized by reaction of adenine and 1,2-Propanediolcyclic carbonate.Four kinds of catalysts were researched and compared during the preparation of conpound (3) from(1) and(2) by condensation.Results:The best catalyst is lithium tert- butoxide which was dissolved in anhydrous DMF solution,and reduce costs and pollution in the process of production. Conclusion:Synthesized(3),the yield increased to 40.5%.更多还原