Ro-31-7453
Chemical Name: 3-(1-Methyl-1H-indol-3-yl)-4-(1-methyl-6-nitro-1H-indol-3-yl)-1H-pyrrole-2,5-dione
CAS No. 125313-92-0
项目整合开发状态: Phase II
项目研究机构: Roche (Originator)
合成路线:6-Nitroindole (I) was methylated using iodomethane and NaH and the resulting 1-methyl-6-nitroindole (II) was acylated with oxalyl chloride in dichloromethane to furnish the glyoxylyl chloride (III).Subsequent condensation of (III) with 1-methylindole-3-acetic acid (IV) in the presence of Et3N gave the bisindolylmaleic anhydride (V).This was finally converted into the target maleimide by heating with ammonia in aqueous DMF in a sealed vessel at 140 C.
📌 参考资料/链接：
参考文献标题:Substd.pyrroles
文献作者:Davis,P.D.; Hill,C.H.; Lawton,G.(F.Hoffmann-La Roche AG)
参考来源:AU 8929658; EP 0328026; JP 1989233281; US 5057614
📄 详细内容
合成路线:6-Nitroindole (I) was methylated using iodomethane and NaH and the resulting 1-methyl-6-nitroindole (II) was acylated with oxalyl chloride in dichloromethane to furnish the glyoxylyl chloride (III).Subsequent condensation of (III) with 1-methylindole-3-acetic acid (IV) in the presence of Et3N gave the bisindolylmaleic anhydride (V).This was finally converted into the target maleimide by heating with ammonia in aqueous DMF in a sealed vessel at 140 C.
参考文献标题:Inhibitors of protein kinase C.1.2,3-Bisarylmaleimides
文献作者:Davis,P.D.; Hill,C.H.; Lawton,G.; Nixon,J.S.; Wilkinson,S.E.; Hurst,S.A.; Keech,E.; Turner,S.E.
参考来源:J Med Chem 1992,35(1),177
产品链接: CAS No. 125313-92-0››