NGB-2904
Chemical Name: N-[4-[4-(2,3-Dichlorophenyl)piperazin-1-yl]butyl]fluorene-2-carboxamide
CAS No. 189061-11-8 (monoHCl)
项目整合开发状态: Biological Testing
项目研究机构: Neurogen (Originator)
合成路线:Dichlorophenylpiperazine (III) was prepared from aniline (I) by dehydrative cyclization with diethanolamine (II) in the presence of P2O5 and Et3N-HCl at 200 C.Alkylation of piperazine (III) with N-(4-bromobutyl) phthalimide (IV) gave (V),and subsequent hydrazinolysis of the phthalimide provided the (4-aminobutyl)piperazine (VI).Finally,condensation of (VI) with fluorene-2-carboxylic acid (VII) yielded the target amide.
📌 参考资料/链接：
参考文献标题:Novel N-aminoalkylfluorenecarboxamides; a new class of dopamine receptor subtype specific ligands
文献作者:Yuan,J.; Chen,X.(Neurogen Corp.)
参考来源:EP 0873329; JP 1998511114; US 5659033; WO 9710229
📄 详细内容
合成路线:Dichlorophenylpiperazine (III) was prepared from aniline (I) by dehydrative cyclization with diethanolamine (II) in the presence of P2O5 and Et3N-HCl at 200 C.Alkylation of piperazine (III) with N-(4-bromobutyl) phthalimide (IV) gave (V),and subsequent hydrazinolysis of the phthalimide provided the (4-aminobutyl)piperazine (VI).Finally,condensation of (VI) with fluorene-2-carboxylic acid (VII) yielded the target amide.
合成路线:Dichlorophenylpiperazine (III) was prepared from aniline (I) by dehydrative cyclization with diethanolamine (II) in the presence of P2O5 and Et3N-HCl at 200 C.Alkylation of piperazine (III) with N-(4-bromobutyl) phthalimide (IV) gave (V),and subsequent hydrazinolysis of the phthalimide provided the (4-aminobutyl)piperazine (VI).Finally,condensation of (VI) with biphenylene-2-carboxylic acid (VII) yielded the target amide.
参考文献标题:NGB 2904 and NGB 2849: Two highly selective dopamine D3 receptor antagonists
文献作者:Yuan,J.; Chen,X.; Brodbeck,R.; Primus,R.; Braun,J.; Wasley,W.F.; Thurkauf,A.
参考来源:Bioorg Med Chem Lett 1998,8(19),2715
产品链接: CAS No. 189061-11-8››