摘要
目的合成新型非甾体抗炎药环氧化酶 2和 5 脂氧合酶双重抑制剂darbufelonemesilate。方法以 2 ,6 二叔丁基 4 甲基苯酚为起始原料 ,经 3步反应制得目标化合物 ,其结构经1H NMR谱和MS谱确证。结果对各步反应条件进行了优化 ,总收率达到 5 2 6 % ,较文献收率提高 2 0 %。结论合成路线简便可行 。
Aim To synthesize darbufelone mesilate ,a new nonster oidal anti-inflammatory drug.Method The target compound was prepare d through a three-step reaction from 2,6-di-tert-butyl-4-methyl phenol .Its structure was con firmed by 1H-NMR and MS.Result The reaction method was imp roved and the total yield was 58.1%,which was 20% higher than that reported in the literature. Conclusion The synthetic route is convenient for the darbufelone mesilate synthesis and the process may be used in industry.
出处
《中国药物化学杂志》
CAS
CSCD
2004年第5期298-300,M005,共4页
Chinese Journal of Medicinal Chemistry