钙通道阻滞剂1,4-二氢吡啶类药物的绿色合成

Green synthesis of 1,4-dihydropyridine drugs as calcium channel blockers

心脏及心脑血管疾病是发达国家人群的第一死因,也是中国人死亡的首位原因.L-型钙通道是目前临床上主要使用选择性钙通道阻滞剂1,4-二氢吡啶类药物.文章研究了在非均相催化剂离子交换树脂Amberlyst 15的催化以及无溶剂条件下,高效的合成了钙通道阻滞剂1,4-二氢吡啶类药物.该反应体系具有原料便宜、反应时间短、操作及后处理简单、催化剂可回收利用、反应可放大等优良特点.

Heart and cardio cerebral vascular disease is the first cause of death in developed countries,and also the first cause of death in China.L-type Calcium channel is a kind of 1,4-dihydropyridine drugs,which are mainly used as selective calcium channel blockers in clinic.An efficient protocol has been developed to synthesize various 1,4-dihydropyridines derivatives using commercially available Amberlyst-15 as a catalyst under solvent-free condition.This process has many merits,such as commercially available catalysts with low cost,quite broad substrate scope,high yields,large-scale preparation,environmental friendliness,easy recovery,and simple work-up procedure.