摘要
目的:改进瑞加德松的合成工艺,提高收率与质量,获得良好的生产工艺。方法:以2-氯腺苷的羟基为原料,经叔丁基二甲基硅烷保护,与水合肼反应得2’,3’,5’-三叔丁基二甲基硅氧基-2-肼基腺苷,再和2-甲酰基-3-氧代丙酸乙酯环合后经甲胺化得带保护的瑞加德松,最后脱去保护基得到瑞加德松。结果 :产品纯度和收率分别提高到99.0%和47.2%。结论 :优化后工艺收率高,产品质量好,操作简便,适合工业化生产。
Objective： To improve the process for the synthesis ofregadenoson and its quality. Methods： Regadenoson was synthesized from 2-chloroadenosine via etherification with t-butyldimethylchlorosilane, reaction with hydrazine hydrate to give 2＇,3＇,5＇-tri-（tert-butyldimethylsiyl）oxy-2-hydrazinyl adenosine, which was cyclized with ethyl 2-formyl-3-oxopropanoate, and finally the protecting groups were removed. Results： The purity and yield of regadenoson were improved up to 99.0% and 47.2%, respectively. Conclusion： The improved process can be easily operated with high yield and quality, and is suitable to industrial production.
出处
《上海医药》
CAS
2016年第3期73-75,共3页
Shanghai Medical & Pharmaceutical Journal
关键词
瑞加德松
合成
工艺改进
纯化
regadenoson
synthesis
process improvement
purification
