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%。
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%.
基金
山东省自然科学基金(Y2008B27)
山东省优秀中青年科学家科研奖励基金(2007BS04021)
