[1]严楠,芮培欣,熊斌,等.韦瑞德合成工艺的优化[J].江西师范大学学报(自然科学版),2014,(04):331-335.
　YAN Nan,RUI Pei-xin,XIONG Bin,et al.The Process OPtinization for the Synthesis of Viread[J].Journal of Jiangxi Normal University:Natural Science Edition,2014,(04):331-335.
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韦瑞德合成工艺的优化()
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《江西师范大学学报》（自然科学版）[ISSN:1006-6977/CN:61-1281/TN]

卷:
期数:
2014年04期
页码:
331-335
栏目:
出版日期:
2014-08-31

文章信息/Info

Title:
The Process OPtinization for the Synthesis of Viread
作者:
严楠;芮培欣;熊斌;刘德永;林春花;廖维林
江西师范大学江西省精细化工重点实验室; 国家单糖化学合成工程技术研究中心，江西 南昌 330027；江西师范大学江西省精细化工重点实验室；国家单糖化学合成工程技术研究中心,江西 南昌,330027
Author(s):
YAN Nan；RUI Pei-xin；XIONG Bin；LIU De-yong；LIN Chun-hua；LIAO Wei-lin
关键词:
(R)-9-(2-羟基丙基)腺嘌呤; 替诺福韦; 合成; 韦瑞德
Keywords:
(R)-9-(2-hydroxypropyl)adenine; tenofovir; synthesis; Viread
分类号:
O626；TQ463.53
文献标志码:
A
摘要:
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.
Abstract:
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.

参考文献/References:

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备注/Memo

备注/Memo:
国家科技支撑计划(2009BAI75B02)；江西省研究生创新专项基金(YC10A051)
更新日期/Last Update: 1900-01-01