CAS: 1166227-08-2; (S)-N1-(2-(Tert-Butyl)-4'-Methyl-[4,5'-Bithiazol]-2'-yl)Pyrrolidine-1,2-Dicarboxamide

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上下游产品

imidazole-1-carboxylic acid (2-tert-butyl-4'-methyl-[4,5']bithiazolyl-2'-yl)-amide L-prolinamide 5-acetyl-2-(N-acetylamino)-4-methylthiazole 1,1'-carbonyldiimidazole

合成工艺路线路线简述

    N-(5-Acetyl-4-Methylthiazol-2-yl)Acetamide置于盐酸,溴体系中,用 1,4-二氧六环,乙醇 用作溶剂,化学反应 93.0H,反应生成A 66; (2S)-N1-(2-叔丁基-4'-甲基[4,5'-联噻唑]-2'-基)-1,2-吡咯烷二甲酰胺
    参考文献:Identification And Optimisation Of A 4',5-Bisthiazole Series Of Selective Phosphatidylinositol-3 Kinase Alpha Inhibitors
    标题:Identification And Optimisation Of A 4',5-Bisthiazole Series Of Selective Phosphatidylinositol-3 Kinase Alpha Inhibitors
    摘要:Exploring The Affinity-Pocket Binding Moiety Of A 2-Aminothiazole (S)-Proline-Amide-Urea Series Of Selective Pi3K Alpha Inhibitors Using A Parallel-Synthesis Approach Led To The Identification Of A Novel 4',5-Bisthiazole Sub-Series. The Synthesis And Optimisation Of Both The Affinity Pocket And (S)-Proline Amide Moieties Within This 4',5-Bisthiazole Sub-Series Are Described. From This Work A Number Of Analogues,Including 14 (A66) And 24,Were Identified As Potent And Selective Pi3K Alpha Inhibitor In Vitro Tool Compounds. (C) 2015 Elsevier Ltd. All Rights Reserved.
    Doi:10.1016/j.Bmcl.2015.06.078

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    主要参考文献


    1: Sweetlove M, Wrightson E, Kolekar S, Rewcastle GW, Baguley BC, Shepherd PR, Jamieson SM. Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth. Front Oncol. 2015 Jun 16;5:135. doi: 10.3389/fonc.2015.00135. eCollection 2015.
    2: Ni Y, Sinnett-Smith J, Young SH, Rozengurt E. PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors. PLoS One. 2013 Sep 9;8(9):e73149. doi: 10.1371/journal.pone.0073149. eCollection 2013. Erratum in: PLoS One. 2014;9(1). doi:10.1371/annotation/70d3c7b0-9718-4bb1-abed-d0defc3b7fc4.
    3: Buchanan CM, Dickson JM, Lee WJ, Guthridge MA, Kendall JD, Shepherd PR. Oncogenic mutations of p110α isoform of PI 3-kinase upregulate its protein kinase activity. PLoS One. 2013 Aug 1;8(8):e71337. doi: 10.1371/journal.pone.0071337. Print 2013.

    合成参考文献


    参考文献:10.1021/ml500354e
    摘要:Mountford SJ, Zheng Z, Sundaram K, Jennings IG, Hamilton JR, Thompson PE. Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. ACS Med Chem Lett. 2015 Jan 08;6(1):3–6.
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