石菖蒲有效成分α-细辛脑的合成  

Synthesis of α-asarone,an active ingredient of Acorus gramineus

作　　者：陈毅平 CHEN Yi-ping(School of Pharmaceutical Science,Guangxi University of Chinese Medicine,Nanning 530200,China)

机构地区：[1]广西中医药大学药学院,广西南宁530200

出　　处：《中国药物化学杂志》2020年第8期477-480,共4页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(81460528,21762010);广西自然科学基金项目(2018GXNSFAA281135,2013 GXNSFAA 019178);广西科技攻关项目(桂科攻0023012);广西教育厅科研项目(桂教科研【2001】401号-85)

摘　　要：目的改进α-细辛脑的合成工艺,提高反应收率,优化产品质量和纯度。方法以1,2,4-三甲氧基苯为原料,经Friedel-Crafts酰基化、还原和脱水反应制备α-细辛脑。结果与结论目标化合物结构经IR、MS、NMR谱确证,总收率由61%提高至85.2%,纯度大于99.9%。优化后的合成方法原料易得、所用催化剂价格低廉、溶剂绿色无污染、操作简便,适合工业化生产。α-Asarone is a naturally occurring compound,which is mainly used in the treatment of bronchitis and asthma.In this study,α-asarone was synthesized from 1,2,4-trimethoxybenzene and propionic acid via Friedel-Crafts acylation,reduction and dehydration reaction,with a purity of 99.9%.The total yield ofα-asarone was increased from 61%to 85.2%.This structure of the product was confirmed by IR,NMR and MS.This method has the advantages of easily available raw materials,low-cost catalyst,green solvent and simplified operational procedure,which is more suitable for industrial production■.

关 键 词：Α-细辛脑 1 2 4-三甲氧基苯 FRIEDEL-CRAFTS酰基化反应 合成 

分 类 号：R914[医药卫生—药物化学]