反式(α)-细辛脑具有平喘、止咳、祛痰、镇静、解痉、抗惊厥及抗癌的药理活性，医学临床应用广泛。反式(α)-细辛脑在天然植物中含量低导致提取纯品困难，化学合成法是有效的制备途径。主要的合成路线有：以1,2,4-三甲氧基苯为原料经酰化、还原及脱水反应得到；以细辛醛为原料经还原和脱水反应制备；以氢醌为原料经氧化、三乙酰化、甲基化、甲酰化和脱水反应后即可得到反式(α)-细辛脑；以 erythro-2-甲基-3羟基-3苯丙酸为原料经立体选择合成直接得到目的产物。反式(α)-细辛脑的分离纯化主要有柱层层析的物理方法和催化异构的化学方法。%Trans (alpha)-asarone has the pharmacological activity of cough, removing phlegm and preventing asthma, sedative, anticonvulsant and anti-cancer, and the clinical application of which is extensively. There are many difficulties in the extraction ofα-asarone due to the low content in the natural plant, thus, the method of chemical synthesis is an effective way of preparingα-asarone. The main synthesis methods are: theα-asarone is obtained by acylation, reduction and dehydration reaction with 1,2,4- trimethoxy benzene as the raw material; theα-asarone is obtained by reduction and dehydration reaction, taking asarum aldehyde as raw material; theα-asarone is obtained by oxidation, three acetylation methyl, formylation and dehydration reaction, using hydroquinone as raw materials; theα-asarone is obtained with erythro-2- methyl -3 hydroxy -3 phenyl propionic acid as raw materials by stereoselective synthesis. The seperation ofα-asarone includes physical separation method of layer chromatography column and the chemical separation method of catalytic isomerization.
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