【摘要】 目的 对从芸香科植物芸香中分离得到的抗肾纤维化活性天然产物香草木宁进行化学全合成研究，以实现大规模制备。方法　该合成路线使用廉价的市售化工材料3，4-二甲氧基苯胺为起始原料，经缩合、加热环化、氯代、氢化还原、脱水消除和烷氧取代六步反应合成得到香草木宁。结果 最终得香草木宁的总产率为25%，纯度大于95%。结论 本文完成了香草木宁的克级规模首次化学合成，且六步反应仅通过单次柱层析纯化即得天然产物纯品，方法成本低、简单易行、绿色高效，为大规模制备香草木宁提供了新方法，为后续香草木宁的药物开发奠定了基础。更多还原

【Abstract】 Objective To achieve large-scale total synthesis of the anti-renal fibrosis compound kokusaginine,which is isolated from Ruta graveolens L.(Rutaceae).Methods The synthesis route used inexpensive and commercially available chemical material,3,4-dimethoxyaniline,as the starting compound.The synthesis involved six steps:condensation,thermal cyclization,chlorination,hydrogenation-reduction,dehydration-elimination,and alkoxy substitution.Results Finally the total yield of kokusaginine was 25%,with purity higher than 95%.Conclusion This study has successfully achieved the first chemical synthesis of kokusaginine on a gram scale.Notably,the six-step reaction yields the pure natural product through a single round of column chromatography.This method is cost-effective,straightforward,and environmentally friendly,providing a new approach for the large-scale production of kokusaginine and future drug development.更多还原