Liguzinediol的合成  

Synthesis of Liguzinediol

作　　者：周莹[1] 李伟[1] 陈磊[1] 陈施伟 王天麟[1] 

机构地区：[1]南京中医药大学药学院,江苏南京210023

出　　处：《中国医药工业杂志》2014年第3期210-211,共2页Chinese Journal of Pharmaceuticals

基　　金：国家自然科学基金(81072542);江苏省自然科学基金(BK2011077);高等学位博士学科点专项基金(20123237110010)

摘　　要：Liguzinediol(1),化学名为2,5-二羟甲基-3,6-二甲基吡嗪,对正常以及急、慢性心力衰竭模型大鼠心脏具有较强的正性肌力作用,且无心律失常等不良反应[1-4]。1可通过作用于心肌细胞内的SERCA2a靶点发挥正性肌力作用[5]。研究表明[6-8],2,5-Dimethylpyrazine was catalyzed by sulfuric acid to form pyrazine ring radical which in turn substitued rapidly by hydroxymethyl radical, which obtained by treatment of methanol with hydrogen peroxide-ferrous sulfate, to yiled liguzinediol as cardiac agent. Optimal conditions were as follows： the molar ratio of 2,5-dimethylpyrazine, CH3OH, 30% H2SO4, FeSO4·7H2O and 30% H2O2 was 1 ： 74 ： 17 ： 2.3 ： 7, the addition of hydrogen peroxide and ferrous sulfate was controlled at the same time with the same speed, and the reaction temperature was 30 - 60℃ mediated by the dropping-speed. The yield was about 31%.

关 键 词：LIGUZINEDIOL radical reaction HYDROXYMETHYLATION SYNTHESIS 

分 类 号：R972.1[医药卫生—药品]