NGB-2849
Chemical Name: N-[4-[4-(2,3-Dichlorophenyl)piperazin-1-yl]butyl]biphenylene-2-carboxamide
CAS No. 198555-28-1
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.
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.
📌 参考资料/链接:
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