| 陈家宝,陈建军,熊霜雨,王周玉,宋巧,钱珊.化学通报,2021,84(9):964-970,980. |
| 连续流微通道反应技术在合成黄酮类天然产物中的应用研究 |
| Research on the Application of Continuous Flow Microchannel Reaction Technology in the Synthesis of Flavonoid Compounds |
| 投稿时间：2021-01-25 修订日期：2021-02-10 |
| DOI： |
| 中文关键词: 连续流微反应 黄酮 二氢黄酮 地奥司明 合成工艺 |
| 英文关键词:Continuous flow microchannel reaction flavone dihydro-flavone diosmin synthesis technology |
| 基金项目:国家自然科学基金项目(81973189)、四川省重点研发项目(19ZDYF0890,21ZDYF3267)、四川省杰出青年科技人才项目(2020JDJQ0054)、西华大学西华学者项目、西华杯和研究生创新基金资助 |
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| 中文摘要: |
| 本文采用连续流微通道反应技术，通过碘介导的二氢黄酮的氧化反应对黄酮类化合物半合成工艺进行了研究。首先选择黄酮类代表药物地奥司明为研究对象，通过连续流微通道反应器分别考察了在常压和背压条件下不同反应条件的影响，实现橙皮苷转化率98%，产品地奥司明收率90%。然后，采用连续流微通道反应完成了多种黄酮、黄酮醇和异黄酮类天然产物的合成。本文研究的黄酮类天然产物的连续流微通道反应工艺，不仅实现了与传统工艺相当的转化率和收率，而且反应时间从传统工艺的8~20小时缩短到2~3 min，反应过程更加安全、高效和快捷，同时拓展了连续流微通道反应技术在药物合成领域的应用范围。 |
| 英文摘要: |
| continuous flow microchannel reactive technology was used to research the semi-synthesis of the flavonoid compounds via iodine-mediated oxidation. Firstly, the synthetic methods of a flavonoid compound diosmin were firstly investigated through the continuous flow microchannel reactor with normal pressure and back pressure, respectively. The optimized continuous flow microchannel reactive conditions were thus obtained, and the conversive rate of the starting material hesperidin reached 98% and the yield of the product diosmin reached 90%. Then, the other flavonoid compounds included flavonoids, flavonols and isoflavones were successfully synthesized. The continuous flow microchannel reactive technology has not only achieved the conversive rate and yield equivalent to those of the traditional process, but also reduces the reaction time from 8~20 hours to 2~3 min. The reactive process became safer, faster and more efficient. The application of continuous flow microchannel reactive technology in pharmaceutical synthesis was further expanded. |
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