摘要
以 2 -溴吡啶为原料 ,采用两种不同的路线合成马来酸罗格列酮 ,总收率分别为 1 5%和1 7%.实验表明 ,经由 Meerwin芳基化反应的途径具有反应原料来源方便易得 ,而经由Knoevenagel缩合反应的途径具有合成路线较短等特点 .关键中间体及最终化合物的结构经元素分析、质谱、核磁共振氢谱及碳谱得到确证 .合成中避免使用高温、高压等条件 。
Rosiglitazone maleate, (a new kind of hypoglycemic drug), (±) 5 [[4 [2 (methyl 2 pyridinylamino)ethoxy]phenyl]methyl] 2,4 thiazolidinedione, was synthesized by two different synthetic routes The total yields were 15% and 17% respectively The route via Meerwin arylation was convenient The route via Knevenagel condensation was simple and short The structure of the intermediates and the target molecule was confirmed by MS, elementary analysis, 1H NMR and 13 C NMR spectra in our experiments The route without high pressure and temperature may be applied to industrial production
出处
《吉林大学自然科学学报》
CAS
CSCD
2000年第3期68-72,共5页
Acta Scientiarum Naturalium Universitatis Jilinensis
关键词
马来酸罗格列酮
Meerwin芳基化
抗糖尿病药
合成
rosiglitazone maleate
Meerwin arylation
Knevenagel condensation
hypoglycemic drug
synthesis
