4-氨基哌啶类化合物的设计、合成及其对单胺递质再摄取的抑制活性

Design,synthesis and monoamine reuptake inhibitors activities of 4-aminopiperidine derivatives

目的设计合成4-氨基哌啶类化合物并研究其对中枢单胺递质（5-HT/NA/DA）的再摄取抑制活性。方法取代的4-氨基哌啶与氯代芳酮进行N-烷基化反应,经成盐制得目标产物Ⅰ1~Ⅰ9,再经硼氢化钠还原、成盐酸盐后制得目标产物Ⅰ10~Ⅰ17;经单胺递质再摄取抑制试验,对目标化合物的活性进行了初步测试。结果与结论共合成了17个未见文献报道的新化合物,经高分辨质谱及核磁共振氢谱确证结构。其中5个化合物对单胺递质再摄取具有一定的抑制活性。

Aim To design and synthesize 4-aminopiperidine derivatives monoamine reuptake inhibitors.Methods The target compounds Ⅰ1-Ⅰ9 were prepared by N-alkylation of 4-aminopiperidine derivatives,and compounds Ⅰ10-Ⅰ17 were obtained by reduction of compounds Ⅰ1-Ⅰ9 with NaBH4.Results and conclusion Seventeen new target compounds were synthesized and their structures were confirmed by HR-MS and 1H-NMR.The results of preliminary pharmacological test showed that five of seventeen compounds possessed diverse monoamine reuptake inhibitors activities.