“一锅法”制备乙酰灯盏乙素苷元  

One-pot synthesis of acetyl scutellarein from scutellarin

作　　者：倪广惠[1,2] 曾忠兰 刘加美 饶高雄 NI Guang-hui ZENG Zhong-lan LIU Jia-mei RAO Gao-xiong(College of Pharmaceutic Science,Yunnan University of Traditional Chinese Medicine,Kunming 650500, China Engineering Laboratory for National Health Theory and Product of Yunnan Province ,Kunming 650500, China)

机构地区：[1]云南中医学院中药学院,云南昆明650500 [2]云南省民族特色养生理论与健康产品工程实验室,云南昆明650500

出　　处：《中国药物化学杂志》2017年第5期379-381,共3页Chinese Journal of Medicinal Chemistry

基　　金：云南省教育厅科学研究基金项目(2015Y314);云南省科技创新强省计划项目(2013AE003)

摘　　要：目的探索制备乙酰灯盏乙素苷元的方法。方法以灯盏乙素为起始原料,与乙酸酐和吡啶共回流,经一步反应获得四乙酰灯盏乙素苷元和部分乙酰化产物6,7,4'-O-三乙酰基灯盏乙素苷元。结果与结论采用"一锅法"合成了乙酰灯盏乙素苷元,总收率在80%以上。乙酰灯盏乙素苷元和其乙酰化产物6,7,4'-O-三乙酰基灯盏乙素苷元均是灯盏乙素结构改造和修饰的重要中间体。与现有的两步合成法相比,本方法具有合成路线短、收率高、反应条件简单等特点,该法为同时获得2个重要中间体提供了有价值的参考。Acetyl scutellarein was an important intermediate in the modification of scutellarin. Acetyl scutel- larein was prepared formerly by two steps,including hydrolysis and acetylation. The total yield was no more than 70% because of the instability of scutellarin under the condition of hydrolysis. Here a one-pot synthesis of acetyl scutellarein from scutellarin was reported. Scutellarin was refluxed with acetic anhydride and pyridine and then purified by silica gel column chromatography to yiled 5,6,7,4＇-O-tetraacetylscutellarein （3） and 6,7,4＇-O-triacetylscutellarein （4）. Both of the two products were important intermediates in the modification of scutellarin. Total yield of the two intermediates was more than 80%.

关 键 词：灯盏乙素苷元 乙酰化 5 6 7 4'-O-四乙酰基灯盏乙素苷元 6 7 4'-O-三乙酰基灯盏乙素苷元 合成 

分 类 号：R284[医药卫生—中药学]