FAUC-327
Chemical Name: 3-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine-7-carbonitrile
项目整合开发状态: Preclinical
项目研究机构: Friedrich-Alexander-Universit鋞 (Originator)
合成路线:Lithiation of 8-azaindole (I) with n-BuLi,followed by treatment with 1,2-diiodoethane (II) affords 7-iodopyrazolopyridine (III),which is then treated with CuCN,Pd2(dba)3 and diphenylphosphinoferrocene (dppf) in refluxing dioxane to provide pyrazolo[1,5-a]pyridine-7-carbonitrile (IV).Finally,Mannich condensation of (IV) with N-(4-chlorophenyl)piperazine (V) and formaldehyde gives rise to the title piperazinomethyl derivative.
📌 参考资料/链接：
参考文献标题:Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: Synthesis,dopamine receptor binding and ligand efficacy
文献作者:L鯾er,S.; Aboul-Fadl,T.; H黚ner,H.; Gmeiner,P.
参考来源:Bioorg Med Chem Lett 2002,12(4),633
📄 详细内容
合成路线:Lithiation of 8-azaindole (I) with n-BuLi,followed by treatment with 1,2-diiodoethane (II) affords 7-iodopyrazolopyridine (III),which is then treated with CuCN,Pd2(dba)3 and diphenylphosphinoferrocene (dppf) in refluxing dioxane to provide pyrazolo[1,5-a]pyridine-7-carbonitrile (IV).Finally,Mannich condensation of (IV) with N-(4-chlorophenyl)piperazine (V) and formaldehyde gives rise to the title piperazinomethyl derivative.
参考文献标题:Effective and variable functionalization of pyrazolo[1,5-a]pyridines involving palladium-catalyzed coupling reactions
文献作者:Aboul-Fadl,T.; L鯾er,S.; Gmeiner,P.
参考来源:Synthesis 2000,12(Suppl.3),1727-1732