| 富马酸替诺福韦二吡呋酯的合成 |
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| 引用本文： | 严楠,林春花,熊云奎,夏剑辉,廖维林.富马酸替诺福韦二吡呋酯的合成[J].精细化工,2014,31(8):983-987. |
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| 作者姓名： | 严楠 林春花 熊云奎 夏剑辉 廖维林 |
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| 作者单位： | 江西师范大学 国家单糖化学合成工程技术研究中心,江西师范大学江西省精细化工重点,江西师范大学江西省精细化工重点实验室,江西师范大学国家单糖化学合成工程技术研究中心,江西师范大学国家单糖化学合成工程技术研究中心 |
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| 基金项目： | 国家科技支撑计划（2009BAI75B02）资助项目 |
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| 摘 要： | 该文对以R-碳酸丙烯酯为原料的富马酸替诺福韦二吡呋酯合成工艺进行了改进。改进的反应步骤是采用微波辅助盐酸加快磷酸酯水解,乙醇镁促进烷基化反应,和碘甲基碳酸异丙酯作为有效酯化试剂。改进后的合成工艺总收率从24%提高到33.5%。并且对环境污染较少和总成本较低,适合于工业化生产。
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| 关 键 词： | 碘甲基碳酸异丙酯 富马酸替诺福韦二吡呋酯 微波辅助 医药与日化原料 |
| 收稿时间： | 2014/3/16 0:00:00 |
| 修稿时间： | 2014/5/27 0:00:00 |
Synthesis of Tenofovir Disoproxil Fumarate |
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| yannan,Lin Chun-hu,xiong yun kui,xia jian hui and liao wei lin.Synthesis of Tenofovir Disoproxil Fumarate[J].Fine Chemicals,2014,31(8):983-987. |
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| Authors: | yannan Lin Chun-hu xiong yun kui xia jian hui and liao wei lin |
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| Affiliation: | Fine Chemical Key Laborary of JiangXi Province, Jiangxi Normal University,Fine Chemical Key Laborary of JiangXi Province, Jiangxi Normal University,National Monosaccharide Chemical Synthesis Engineering Research Center , Jiangxi Normal University,National Monosaccharide Chemical Synthesis Engineering Research Center , Jiangxi Normal University |
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| Abstract: | In this paper, process improvements of the synthesis of Tenofovir disoproxil fumarate started from (R)-propylene carbonate was optimized. The process improvements were included in simply microwave-assisted acid hydrolysis of phosphonate ester, alkylation promoted with magnesium ethoxide, and iodine methyl isopropyl carbonate as an efficiently esterification reagent. The overall yield of the process of synthesis of Tenofovir disoproxil fumarate was not only improved from 24% to 33.5%, but also the identified process were more environmentally friendly, lower cost, and more suitable for productive and robust production. |
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| Keywords: | 1-Iodomethylisopropyl Carbonate Tenofovir Disoproxil Fumarate Microwave-assisted |
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