江西师范大学学报（自然科学版）
江西師範大學學報（自然科學版）
강서사범대학학보（자연과학판）
JOURNAL OF JIANGXI NORMAL UNIVERSITY（NATURAL SCIENCES EDITION）
2014年
4期
331-335
,共5页
严楠%芮培欣%熊斌%刘德永%林春花%廖维林
嚴楠%芮培訢%熊斌%劉德永%林春花%廖維林
엄남%예배흔%웅빈%류덕영%림춘화%료유림
(R)-9-(2-羟基丙基)腺嘌呤%替诺福韦%合成%韦瑞德
(R)-9-(2-羥基丙基)腺嘌呤%替諾福韋%閤成%韋瑞德
(R)-9-(2-간기병기)선표령%체낙복위%합성%위서덕
(R)-9-(2-hydroxypropyl)adenine%tenofovir%synthesis%Viread
对韦瑞德合成工艺进行优化.以腺嘌呤为起始原料，将其与 R-碳酸丙烯酯缩合反应制得（R）-9-（2-羟基丙基）腺嘌呤，经醚化、超声辅助三甲基氯硅烷脱磷酸酯得到替诺福韦，再经碘甲基碳酸异丙酯酯化、成盐得到最终产物韦瑞德，总收率为31%（以腺嘌呤计算），HPLC 纯度达99.5%.该优化合成工艺成本低廉，收率高，步骤短，适合于工业化生产.
對韋瑞德閤成工藝進行優化.以腺嘌呤為起始原料，將其與 R-碳痠丙烯酯縮閤反應製得（R）-9-（2-羥基丙基）腺嘌呤，經醚化、超聲輔助三甲基氯硅烷脫燐痠酯得到替諾福韋，再經碘甲基碳痠異丙酯酯化、成鹽得到最終產物韋瑞德，總收率為31%（以腺嘌呤計算），HPLC 純度達99.5%.該優化閤成工藝成本低廉，收率高，步驟短，適閤于工業化生產.
대위서덕합성공예진행우화.이선표령위기시원료，장기여 R-탄산병희지축합반응제득（R）-9-（2-간기병기）선표령，경미화、초성보조삼갑기록규완탈린산지득도체낙복위，재경전갑기탄산이병지지화、성염득도최종산물위서덕，총수솔위31%（이선표령계산），HPLC 순도체99.5%.해우화합성공예성본저렴，수솔고，보취단，괄합우공업화생산.
The method for the synthesis of Viread was studied. The target product was synthesized from adenine via ring-opening condensation with(R)-propylene carbonate,etherification and ultrasonic radiation-assisted hydrolysis to give Tenofovir. Which was subjected to reaction with Iodine methyl isopropyl carbonate,followed by salt formation with an overall yield of about 31% ,the HPLC purity was up to 99. 5% . The optimized synthetic process has the ad-vantages of cheapness,high yield,simple and easy work-up. Which was more suitable for industrialized production.
