LY-402913
Chemical Name: 2-[3-(9-Chloro-3-methyl-4-oxo-4,5-dihydroisoxazolo[4,3-c]quinolin-5-yl)phenyl]-N-(3,4,5-trimethoxyphenyl)acetamide
CAS No. 246238-55-1
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线:Condensation of 3-(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolecarbonyl chloride (I) with methyl 3-aminophenylacetate (II) leads to amide (III).Intramolecular cyclization of (III) and simultaneous hydrolysis in the presence of NaOH in MeOH/DMF provide the isoxazoloquinoline derivative (IV).After activation of acid (IV) as the corresponding acid chloride (V),coupling with 3,4,5-trimethoxyaniline (VI) furnishes the title compound
📌 参考资料/链接：
参考文献标题:Methods for inhibiting MRP1
文献作者:Kroin,J.S.; Norman,B.H.; Gruber,J.M.(Eli Lilly and Company)
参考来源:EP 1067928; JP 2002510625; US 6369070; WO 9951228
📄 详细内容
合成路线:Condensation of 3-(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolecarbonyl chloride (I) with methyl 3-aminophenylacetate (II) leads to amide (III).Intramolecular cyclization of (III) and simultaneous hydrolysis in the presence of NaOH in MeOH/DMF provide the isoxazoloquinoline derivative (IV).After activation of acid (IV) as the corresponding acid chloride (V),coupling with 3,4,5-trimethoxyaniline (VI) furnishes the title compound
参考文献标题:Tricyclic isoxazoles are novel inhibitors of the multidrug resistance protein (MRP1)
文献作者:Norman,B.H.; Gruber,J.M.; Hollinshead,S.P.; Wilson,J.W.; Starling,J.J.; Law,K.L.; Self,T.D.; Tabas,L.B.; Williams,D.C.; Paul,D.C.; Wagner,M.M.; Dantzig,A.H.
参考来源:Bioorg Med Chem Lett 2002,12(6),883
产品链接: CAS No. 246238-55-1››