溶剂对二萜生物碱结构的影响  

Effects of solvent on the structures of diterpenoid alkaloids

作　　者：邹娇 时嘉敏 何翠林 刘兴鸿 陈东林[1] ZOU Jiao;SHI Jiamin;HE Cuilin;LIU Xinghong;CHEN Donglin(West China School of Pharmacy,Sichuan University,Chengdu,Sichuan,610041 P.R.China)

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2020年第2期127-130,共4页West China Journal of Pharmaceutical Sciences

摘　　要：目的研究含8-OAc的二萜生物碱在甲醇、乙醇、正丁醇溶剂中的C-8位的烷氧取代反应。方法以常见的二萜生物碱乌头碱、3-去氧乌头碱、滇乌碱和草乌甲素为底物,使用甲醇、乙醇或正丁醇为溶剂,进行回流反应。结果通过回流反应,成功制得乌头碱、3-去氧乌头碱、滇乌碱和草乌甲素的C-8位烷氧基取代的化合物。结论 C-8位为乙酰氧基取代的二萜生物碱在甲醇、乙醇或正丁醇等醇溶剂中加热回流时,易通过Grob裂解发生C-8位的烷氧取代反应,但酸性环境可抑制该反应的发生。OBJECTIVE To study the alkoxy substitution at C-8 of diterpenoid alkaloids containing 8-OAc in methanol,ethanol or n-butanol solvents.METHODS The common diterpenoid alkaloids:Aconitine,3-deoxyaconitine,yunaconitine and crassicauline A were used as substrates,and methanol,ethanol or n-butanol were used as solvent for the reflux reaction.RESULTS The alkoxy substituted compounds at the C-8 of aconitine,3-deoxyaconitine,yunaconitine and crassicauline A were successfully obtained by reflux reaction.CONCLUSION When the acetoxy-substituted diterpenoid alkaloids in the C-8 were refluxed in alcohol solvents such as methanol,ethanol or n-butanol,the alkoxy substitution reaction at C-8 can easily occur through Grob cleavage,but the acid environment can inhibit the occurrence of the reaction.

关 键 词：二萜生物碱 乌头碱 3-去氧乌头碱 滇乌碱 草乌甲素 C-8位烷氧基取代 Grob裂解 酸性溶剂 

分 类 号：R914[医药卫生—药物化学]