FAUC-213
2-{[4-(4-氯苯基)-1-哌嗪基]甲基}吡唑并[1,5-a]吡啶Chemical Name: 2-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine
CAS No. 337972-47-1
项目整合开发状态: Preclinical
项目研究机构: Friedrich-Alexander-Universit鋞 (Originator)
合成路线:The 1,3-dipolar cycloaddition of N-aminopyridinium iodide (I) to dimethyl acetylenedicarboxylate (II) afforded the pyrazolopyridine system (III).Ester groups hydrolysis and regioselective decarboxylation of (III) with hot 50% sulfuric acid gave the mono-carboxylic acid (IV),which was further esterified with ethanol and sulfuric acid.Finally,reductive amination of the ethyl ester (V) with (p-chlorophenyl)piperazine (VI) in the presence of LiAlH4 provided the target compound.
📌 参考资料/链接:
参考文献标题:Rationally based efficacy tuning of selective dopamine D4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl) piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213)
文献作者:L鯾er,S.; Hubner,H.; Utz,W.; Gmeiner,P.
参考来源:J Med Chem 2001,44(17),2691