中乌头碱的丙酰化修饰研究  

Study on the Method of Mesaconitine Propionylation

作　　者：许源[1] 侯大斌[1] 王惠[1] 袁小红[1] 杨海君[1] 赵祥升[1] 

机构地区：[1]西南科技大学,四川绵阳621010

出　　处：《时珍国医国药》2009年第12期2942-2944,共3页Lishizhen Medicine and Materia Medica Research

基　　金：国家"十一五"科技支撑重大专项课题(No.2006BAE01A01-12)

摘　　要：目的探讨中乌头碱C3,C13,C15位羟基的丙酰化方法。方法以中乌头碱、丙酸酐为原料合成中乌头碱酯化衍生物。结果得到4种丙酰化衍生物,并通过ESI-MS,1H-NMR验证了其结构,分别为3-丙酰基中乌头碱(a);3,13,15-三丙酰基中乌头碱(b);3-丙酰基-13,15-二乙酰基中乌头碱(c);3-乙酰基-13-丙酰基中乌头碱(d)。据文献检索,所有化合物均为首次报道。结论中乌头碱的三个羟基中,C3-OH最易被丙酰化,C15-OH最难被丙酰化。Objective To study the propionylation method of C3-OH,C13-OH,C15-OH from mesaconitine. Methods Esterification derivatives were synthesized from mesaconitine and propionic anhydride. Results Four derivatives were synthesized. They were 3 - propionyl mesaeonitine, 3,13,15-tripropionyl mesaconitine, 3 - propionyl-13, 15-diacetyl mesaeonitine, 3-acetyl-13-propionyl mesaconitine. All the derivatives were reported for the first time recording to literature retrieval, and characterized by ESI-MS, 1H- NMR. Conclusion Among the three hydroxy groups, C3-OH is the first esterified one and the C15-OH is the last esterified one.

关 键 词：乌头 二萜生物碱 酯化反应 植物源农药 

分 类 号：R284.2[医药卫生—中药学]