LY-402913-药物合成数据库

【药物名称】LY-402913

化学结构式(Chemical Structure):

参考文献No.	40785
标题:	Methods for inhibiting MRP1
作者:	Kroin, J.S.; Norman, B.H.; Gruber, J.M. (Eli Lilly and Company)
来源:	EP 1067928; JP 2002510625; US 6369070; WO 9951228

合成路线图解说明: 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No.	666204
标题:	Tricyclic isoxazoles are novel inhibitors of the multidrug resistance protein (MRP1)
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.
来源:	Bioorg Med Chem Lett 2002,12(6),883

合成路线图解说明: 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