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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。
Objective To design and synthesize 4-aminopiperidine compounds and study their reuptake inhibitory activity on central monoamine transmitter (5-HT / NA / DA). The substituted 4-aminopiperidine is reacted with chloroaryl ketone to obtain the target product I1 ~ I9 by salt-formation, and then reduced with sodium borohydride to give the desired product I10 ~ Ⅰ17; After the monoamine neurotransmission reuptake inhibition test, the activity of the target compound was preliminarily tested. RESULTS AND CONCLUSIONS A total of 17 new compounds were reported in the literature, which were confirmed by high-resolution mass and 1H-NMR. Among them, 5 compounds had certain inhibitory activity on monoamine reuptake.