Continuous synthesis of ginkgolide B derivatives in a micro-flow system
作者： Yinlin Qin , Wei He , Mei Su , Zheng Fang , Jiajia Gu
DOI: 10.1016/J.TETLET.2016.02.018
关键词: Iodine 、 Hydrochloride 、 Halide 、 Ginkgolide-B 、 Calcium carbonate 、 Chemistry 、 Nuclear chemistry 、 Flow chemistry 、 Magazine 、 Organic chemistry 、 Ethyl Chloride
摘要: Abstract In this study, etherification process of ginkgolide B in a micro-flow system was investigated. With calcium carbonate as an acid-binding agent, the optimal result obtained such conditions: residence time 3 min, temperature 85 °C, molar ratio to dimethylamino ethyl chloride hydrochloride 1:2, potassium iodide 1:0.2, and 1:2.5. Meanwhile, novel MFS could proceed well for reaction between other halides, afford target products moderate yields. Besides, salification conducted valve assisted micromixer by reacting dimethylaminoethyl with methane sulfonic acid. Compared conventional drugs, enhanced bioavailability when nano-scale drugs were dosed.
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