新产品编号:1940041
Chemical Name: N-(5-Isoquinolinyl)-5-methyl-1-[3-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxamide
项目整合开发状态: Preclinical
项目研究机构: R.W. Johnson (Originator)
合成路线:Cyclization of ethyl 2,4-dioxovalerate (I) with 3-(trifluoromethyl)phenylhydrazine (II) in a refluxing mixture of HOAc and 2-methoxyethanol produced pyrazole ester (III).After saponification of the ethyl ester group of (III),the resulting carboxylic acid (IV) was coupled to 5-aminoisoquinoline (V) by using O-(7-azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate to furnish the corresponding amide.
📌 参考资料/链接：
参考文献标题:Pyrazole carboxamides useful for the treatment of obesity and other disorders
文献作者:Reitz,A.B.; Lovenberg,T.W.; Kordik,C.P.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:WO 0069849
📄 详细内容
合成路线:Cyclization of ethyl 2,4-dioxovalerate (I) with 3-(trifluoromethyl)phenylhydrazine (II) in a refluxing mixture of HOAc and 2-methoxyethanol produced pyrazole ester (III).After saponification of the ethyl ester group of (III),the resulting carboxylic acid (IV) was coupled to 5-aminoisoquinoline (V) by using O-(7-azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate to furnish the corresponding amide.
参考文献标题:Pyrazole-based antagonists of the human neuropeptide-Y5 (NPY5) receptor
文献作者:Kordik,C.P.; Lou,C.; Zanoni,B.; et al.
参考来源:220th ACS Natl Meet (Aug 20 2000,Washington DC) 2000,Abst MEDI 304
合成路线:Cyclization of ethyl 2,4-dioxovalerate (I) with 3-(trifluoromethyl)phenylhydrazine (II) in a refluxing mixture of HOAc and 2-methoxyethanol produced pyrazole ester (III).After saponification of the ethyl ester group of (III),the resulting carboxylic acid (IV) was coupled to 5-aminoisoquinoline (V) by using O-(7-azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate to furnish the corresponding amide.
参考文献标题:Pyrazolecarboxamide human neuropeptide Y5 receptor ligands with in vivo antifeedant activity
文献作者:Kordik,C.P.; Luo,C.; Zanoni,B.C.; Lovenberg,T.W.; Wilson,S.J.; Vaidya,A.H.; Crooke,J.J.; Rosenthal,D.I.; Reitz,A.B.
参考来源:Bioorg Med Chem Lett 2001,11(17),2287