📜2-(二丁氧基甲基)-4-氟-1-硝基苯置于palladium On Activated Charcoal 盐酸,Potassium Tert-Butylate,氢气,Sodium Hydride,Potassium Carbonate,三乙胺体系中,用 四氢呋喃,1,4-二氧六环,甲醇,二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,-78.0~20.0 °C,101.33 Kpa 条件下,反应 19.17H,反应生成 Gsk-3抑制剂(Ly2090314)
参考文献:Substituted 3-Imidazo[1,2-A]Pyridin-3-Yl-4-(1,2,3,4-Tetrahydro-[1,4]Diazepino-[6,7,1-Hi]Indol-7-yl)Pyrrole-2,5-Diones As Highly Selective And Potent Inhibitors Of Glycogen Synthase Kinase-3
标题:Substituted 3-Imidazo[1,2-A]Pyridin-3-Yl-4-(1,2,3,4-Tetrahydro-[1,4]Diazepino-[6,7,1-Hi]Indol-7-yl)Pyrrole-2,5-Diones As Highly Selective And Potent Inhibitors Of Glycogen Synthase Kinase-3
摘要:Glycogen Synthase Kinase-3 (Gsk3) Is Involved In Signaling From The Insulin Receptor. Inhibitors Of Gsk3 Are Expected To Effect Lowering Of Plasma Glucose Similar To Insulin,Making Gsk3 An Attractive Target For The Treatment Of Type 2 Diabetes. Herein We Report The Discovery Of A Series Of Potent And Selective Gsk3 Inhibitors. Compounds 7-12 Show Oral Activity In An In Vivo Model Of Type Ii Diabetes,And 9 And 12 Have Desirable Pk Properties.
DOI:10.1021/jm049768A