2-(E)-亚苄基-5-氨甲基环戊醇乙酯类化合物的合成及抗炎活性研究

Synthesis and Anti-Inflammatory Activity of Esters of 2-(E)-Benzylidene-5-Aminomethylcyclopentanol

以环戊酮为起始原料,通过Stork烯胺反应、Mannich反应、选择性还原及酯化反应,设计合成2-(E)-亚苄基-5-氨甲基环戊醇乙酯类化合物,并以二甲苯致小鼠耳肿胀模型对目标化合物的抗炎活性进行初步评价。共合成了6个化合物,经~1H-NMR、MS确证其结构,初步药理实验结果表明目标化合物保留了抗炎活性。

The target compounds were synthesized from cyclo pentanol via Stork reaction, Mannich condensation, selective reduction and esterification. Xylene-induced mice ear edema assay was used to evaluate the anti-inflammatory activity of the target compounds. Six novel compounds were synthesized and characterized by 1 H-NMR and MS. Preliminary pharmacological text show that the anti-inflammatory activity of target compound is maintained.