新产品编号:585849

3-[1-(3-氨基苯基)-3-叔丁基-1H-吡唑-5-基]-1-(2,3-二氯苯基)脲Chemical Name: N-[1-(3-Aminophenyl)-3-tert-butyl-1H-pyrazol-5-yl]-N'-(2,3-dichlorophenyl)urea
CAS No. 227622-98-2
项目整合开发状态: Preclinical
项目研究机构: Bayer (Originator)
合成路线:Aminopyrazole (III) was prepared by condensation of keto nitrile (I) with 3-nitrophenylhydrazine (II) in ethanolic HOAc.Subsequent reaction of (III) with 2,3-dichlorophenyl isocyanate (IV) in hot toluene produced the urea derivative (V).The nitro group of (V) was finally reduced to the title aniline by means of iron and acetic acid.
📌 参考资料/链接:
参考文献标题:Inhibition of p38 kinase activity using aryl and heteroaryl substd.heterocyclic ureas
文献作者:Redman,A.; Smith,R.A.; Khire,U.; Wood,J.E.; Dumas,J.; Sibley,R.; Lowinger,T.B.; Scott,W.J.; Johnson,J.; Riedl,B.; Hatoum-Mokdad,H.(Bayer AG)
参考来源:WO 9932110

📄 详细内容


合成路线:Aminopyrazole (III) was prepared by condensation of keto nitrile (I) with 3-nitrophenylhydrazine (II) in ethanolic HOAc.Subsequent reaction of (III) with 2,3-dichlorophenyl isocyanate (IV) in hot toluene produced the urea derivative (V).The nitro group of (V) was finally reduced to the title aniline by means of iron and acetic acid.

参考文献标题:Synthesis and SAR of p38 kinase inhibitors from the urea class
文献作者:Dumas,J.; Bobko,M.; Bhargava,A.; et al.
参考来源:220th ACS Natl Meet (Aug 20 2000,Washington DC) 2000,Abst MEDI 148


合成路线:Aminopyrazole (III) was prepared by condensation of keto nitrile (I) with 3-nitrophenylhydrazine (II) in ethanolic HOAc.Subsequent reaction of (III) with 2,3-dichlorophenyl isocyanate (IV) in hot toluene produced the urea derivative (V).The nitro group of (V) was finally reduced to the title aniline by means of iron and acetic acid.

参考文献标题:Pharmacological characterization of pyrazolyl urea p38 kinase inhibitors
文献作者:Ranges,G.E.; Bortolon,E.; Chau,T.; et al.
参考来源:220th ACS Natl Meet (Aug 20 2000,Washington DC) 2000,Abst MEDI 149


合成路线:Aminopyrazole (III) was prepared by condensation of keto nitrile (I) with 3-nitrophenylhydrazine (II) in ethanolic HOAc.Subsequent reaction of (III) with 2,3-dichlorophenyl isocyanate (IV) in hot toluene produced the urea derivative (V).The nitro group of (V) was finally reduced to the title aniline by means of iron and acetic acid.
参考文献标题:1-Phenyl-5-pyrazolyl ureas: Potent and selective p38 kinase inhibitors
文献作者:Dumas,J.; Hatoum-Mokdad,H.; Sibley,R.; Riedl,B.; Scott,W.J.; Monahan,M.K.; Lowinger,T.B.; Brennan,C.; Natero,R.; Turner,T.; Johnson,J.S.; Schoenleber,R.; Bhargava,A.; Wilhelm,S.M.; Housley,T.J.; Ranges,G.E.; Shrikhande,A.
参考来源:Bioorg Med Chem Lett 2000,10(18),2051


产品链接: CAS No. 227622-98-2››