📜1-溴-2-氯乙烷,1-(3-三氟甲基苯基)哌嗪 以 甲苯 作为反应溶剂,化学反应 6.0H,反应生成 1-(2-氯乙基)-4-[3-(三氟甲基)苯基]哌嗪二盐酸盐,氟班色林杂质
参考文献:Synthesis Of New 1,2,3-Benzotriazin-4-One-Arylpiperazine Derivatives As 5-Ht 1A Serotonin Receptor Ligands
标题:Synthesis Of New 1,2,3-Benzotriazin-4-One-Arylpiperazine Derivatives As 5-Ht 1A Serotonin Receptor Ligands
摘要:A Series Of Novel 1,2,3-Benzotriazin-4-One Derivatives Was Prepared And Evaluated As Ligands For 5-Ht Receptors. Radioligand Binding Assays Proved That The Majority Of The Novel Compounds Behaved As Good To Excellent Ligands At The 5-Ht1A Receptor,Some Of Which Were Selective With Respect 5-Ht2A And 5-Ht2C Receptors. Six Analogues (1A,2A,2B,2C,2E And 2I) Were Selected And Further Evaluated For Their Binding Affinities On D-1,D-2 Dopaminergic And Alpha(1)-,Alpha(2)-Adrenergic Receptors. A O-och3 Derivative (2E) Bound At 5-Ht1A Sites With Subnanomolar Affinity (Ic50 = 0.059 Nm) And Shows High Selectivity Over All Considered Receptors And May Offer A New Lead For The Development Of Therapeutically Efficacious Agents. (C) 2000 Elsevier Science Ltd. All Rights Reserved.
DOI:10.1016/s0968-0896(00)00004-3