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梓醇全丙酰化产物的微波合成及其神经保护作用初探

Microwave-Assisted Synthesis of Catalpol Perpropionylated Derivative and Its Neuroprotective Effect

摘要: [目的] 微波辅助合成具有潜在神经保护作用的梓醇全丙酰化产物(CP-6)。 [方法] 以梓醇、丙酰酐为原料,吡啶为溶剂和缚酸剂,微波辅助合成梓醇全丙酰化衍生物。CP-6经FT-IR、HRMS、NMR表征,采用MTT法筛查其神经保护活性。 [结果] 当丙酸酐与梓醇摩尔比为18,微波反应器反应温度 80 ℃,反应时间6 h, 梓醇在吡啶中浓度 25 g/L时梓醇全丙酰化产物产率可达98.51%。CP-6具有潜在的神经保护活性。 [结论] CP-6可经微波合成制得,其具有神经保护作用,是一种潜在的神经保护作用药物。

Abstract: [Objective] Synthesis of potential neroprotective agent catalpol perpropionylated derivative (CP-6), and determination of the optimal microwav-assisted synthesis conditions. [Methods] CP-6 was synthesized by microwave-assisted synthesis (MCAS) using catalpol and propionyl anhydride as raw materials and pyridine as solvent and acid-binding agent. It was characterized by FT-IR, HRMS, NMR and assayed for neuroprotective activity by MTT method. [Results] When the molar ratio of propionic anhydride to catalpol is 18, the concentration of catalol in pyridine is 25 g/L, the reaction temperature of microwave reactor is 80 ℃, and the reaction time is 6 h, the yield of CP-6 can reach 98.51%. CP-6 has potential neroprotective activity."

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[V1] 2020-03-05 17:52:13 ChinaXiv:202003.00024V1 下载全文
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