CAS: 603288-22-8; 3-(9-Fluoro-2-(Piperidine-1-Carbonyl)-1,2,3,4-Tetrahydro-[1,4]Diazepino[6,7,1-Hi]Indol-7-yl)-4-(Imidazo[1,2-A]Pyridin-3-yl)-1H-Pyrrole-2,5-Dione

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piperidine carbamoyl chloride 3-(9-fluoro-1,2,3,4-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-7-yl)-4-imidazo[1,2-a]pyridin-3-yl-pyrrole-2,5-dione hydr°Chloride 2-aminopyridine 2-(imidazo-[1,2-a]pyridin-3-yl)acetamide

合成工艺路线路线简述

    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

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    主要参考文献

    1. A phase I dose-escalation, pharmacokinetic (PK), and pharmacodynamic (PD) evaluation of intravenous LY2090314 a GSK3 inhibitor administered in combination with pemetrexed and carboplatin. Meeting: 2011 ASCO Annual Meeting, Presenter: Les H. Brail.

    合成参考文献


    参考文献:10.1007/s11064-006-9128-5
    摘要:Jope RS, Yuskaitis CJ, Beurel E. Glycogen Synthase Kinase-3 (GSK3): Inflammation, Diseases, and Therapeutics. Neurochemical Research. 2006 Aug 30;32(4-5):577–95. doi: 10.1007/s11064-006-9128-5.
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