化学合成;作为5-HT激动剂，取代大鼠内皮层中5-HT3R的[3H]GR65630的Ki值为1.4 nM；对SARS-CoV-2具有抗病毒活性，EC50值为31.64 μM；在外周模型中表现为5-HT3R的激动剂，可用于神经疾病研究
医药;化学合成
路线1：以乙二醇为溶剂的合成方法
- 原料：无水哌嗪、2-氯喹啉、乙二醇、饱和碳酸氢钠水溶液、氯仿、无水硫酸镁
- 步骤：将4.31g无水哌嗪溶解在30ml乙二醇中，加入818mg 2-氯喹啉，140℃搅拌2小时；冷却后加入饱和碳酸氢钠水溶液，氯仿萃取；有机层用无水硫酸镁干燥，减压蒸馏除溶剂；残渣经硅胶柱色谱（氯仿：甲醇=2：1）精制
- 产率：100%
- 参考文献：[1] Patent: EP1724267, 2006, A1. Location in patent: Page/Page column 35; 68 [2] Journal of Medicinal Chemistry, 2010, vol. 53, # 21, p. 7549 - 7563 [3] Journal of Pharmaceutical Sciences, 1992, vol. 81, # 1, p. 99 - 103 [4] Chemical and Pharmaceutical Bulletin, 2001, vol. 49, # 10, p. 1314 - 1320 [5] Patent: WO2004/46124, 2004, A1. Location in patent: Page 41 [6] European Journal of Medicinal Chemistry, 2015, vol. 98, p. 221 - 236 [7] Patent: WO2008/153325, 2008, A1. Location in patent: Page/Page column 45-46 [8] Polish Journal of Chemistry, 2001, vol. 75, # 1, p. 71 - 78 [9] Bulletin de la Societe Chimique de France, 1929, vol. <4> 45, p. 1177,1178 [10] Patent: US6043247, 2000, A [11] Molecules, 2008, vol. 13, # 10, p. 2426 - 2441 [12] Acta Poloniae Pharmaceutica - Drug Research, 2018, vol. 75, # 4, p. 891 - 901
路线2：以异丙醇为溶剂的合成方法
- 原料：哌嗪、2-氯喹啉、异丙醇、水、乙酸乙酯、饱和氯化钠溶液、无水硫酸镁
- 步骤：氮气保护下，将10.20g哌嗪溶于15mL异丙醇，加入0.20g 2-氯喹啉，加热回流搅拌24小时；反应完成后加水，乙酸乙酯萃取；合并有机层，饱和氯化钠溶液洗涤，无水硫酸镁干燥，减压浓缩；粗产物经硅胶柱色谱（二氯甲烷:甲醇=4:1）纯化
- 产率：36%
- 参考文献：[2] Journal of Medicinal Chemistry, 2010, vol. 53, # 21, p. 7549 - 7563 [3] Journal of Pharmaceutical Sciences, 1992, vol. 81, # 1, p. 99 - 103 [4] Chemical and Pharmaceutical Bulletin, 2001, vol. 49, # 10, p. 1314 - 1320 [5] Patent: WO2004/46124, 2004, A1. Location in patent: Page 41
