摘要
用亚磷酸二乙酯和多聚甲醛经缩合、酯化得到对甲苯磺酸二乙氧基磷酰基甲酯(6)。另用腺嘌呤和碳酸亚乙酯反应得到9-(2-羟乙基)腺嘌呤,与6在NaH作用下缩合后,经水解、酰化等反应制得抗病毒药阿德福韦酯,总收率18%。
Adefovir dipivoxil was synthesized by reaction of adenine and ethylene carbonate to give 9-(hydroxyethyl)adenine,which was subjected to condensation with 4-toluenesulfonic acid diethoxyphosphorylmethyl ester(6)in presence of Nail,hydrolysis and then acylation with an overall yield of 18%(base on adenine).Compound 6 was prepared from diethyl phosphate and paraformaldehyde by condensation and esterification.
作者
蒋晔
徐智儒
张丽芳
张晓青
JIANG Ye;XU Zhi-ru;ZHANG Li-fang;ZHANG Xiao-qing(J.Institute of Pharmacy,Hebei Medical University;Pharmaceutical Factory of Hebei Medical University,Shijiazhuang050017)
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2007年第1期4-6,共3页
Chinese Journal of Pharmaceuticals
关键词
阿德福韦酯
核苷类似物
合成
adefovir dipivoxil
acyclic nucleotide
synthesis
