CAS: 1061353-68-1; 2-((2-((2-Methoxy-4-Morpholinophenyl)Amino)-5-(Trifluoromethyl)Pyridin-4-yl)Amino)-N-Methylbenzamide

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上下游产品

2-methoxy-4-morpholinoaniline 2-((2-chloro-5-(trifluoromethyl)pyridin-4-yl)amino)-N-methylbenzamide PND-1186 hydr°Chloride 2-Amino-N-methylbenzamidPND-1186 hydr°Chloride

合成工艺路线路线简述

    📜2-氯-5-三氟甲基-4-碘吡啶置于palladium Diacetate,R-(+)-1,1'-联萘-2,2'-双二苯膦 盐酸,Caesium Carbonate体系中,用 1,4-二氧六环,水,甲苯 用作溶剂,化学反应 0.42H,反应生成Pnd-1186游离态
    参考文献: Anilinopyridines As Inhibitors Of Fak[fr] Anilinopyridines Utilisées Comme Inhibiteurs De Fak
    标题: Anilinopyridines As Inhibitors Of Fak[fr] Anilinopyridines Utilisées Comme Inhibiteurs De Fak
    摘要:本发明涉及一种化合物的公式(i)或其药用可接受盐,其中r1-R4,Q,Z,R和p如本文所定义.本发明的化合物在治疗与fak过度表达相关的疾病方面具有用途,包括增殖性疾病.

    专利信息


    专利号:US-9505719-B2
    优先权日:2010-06-30
    标 题 :Synthesis and use of kinase inhibitors
    发明人：LEI YIXIONG; BEHRENS CARL HENRY; LI HUI-YIN; SUN CONNIE L
    权利人:VERASTEM INC
    摘要:An improved synthesis of a class of inhibitor of Focal Adhesion Kinase (FAK) is provided, wherein use of an expensive palladium-based catalyst is reduced and reaction yields and product purities are improved. Two key reactions of coupling of aryl halides with anilines are optimized with the surprising discovery that the palladium-based catalyst can be dispensed with entirely in one of the reactions. The invention also provides the use of the FAK-inhibitory compounds in the treatment of inflammatory and immune disorders and of arthritis.

    专利号:WO-2012012139-A1
    优先权日:2010-06-30
    标题:Synthesis and use of kinase inhibitors

    专利号:JP-2013529687-A
    优先权日:2010-06-30
    标 题:Synthesis and use of kinase inhibitors

    专利号:CN-103168037-A
    优先权日:2010-06-30
    标 题 :Synthesis and use of kinase inhibitors

    专利号:US-2014235635-A1
    优先权日:2010-06-30
    标题 :Synthesis and use of kinase inhibitors

    专利号:JP-5923499-B2
    优先权日:2010-06-30
    标 题 :Synthesis and use of kinase inhibitors

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    主要参考文献


    1: Jin B, Wang J, Chen Y, Zuo W, Hong B, Li J, Huang F, Zhang M, Wang Y. Focal adhesion kinase induces cardiac remodeling through NF-κB-mediated inflammatory responses in diabetic cardiomyopathy. Int Immunopharmacol. 2023 Jul;120:110280. doi: 10.1016/j.intimp.2023.110280. Epub 2023 May 20. 14(19):4784. doi: 10.3390/cancers14194784.
    3: Yuen ML, Zhuang L, Rath EM, Yu T, Johnson B, Sarun KH, Wang Y, Kao S, Linton A, Clarke CJ, McCaughan BC, Takahashi K, Lee K, Cheng YY. The Role of E-Cadherin and microRNA on FAK Inhibitor Response in Malignant Pleural Mesothelioma (MPM). Int J Mol Sci. 2021 Sep 23;22(19):10225. doi: 10.3390/ijms221910225.
    4: He J, Zhang S, Qiu Z, Li X, Huang H, Jin W, Xu Y, Shao G, Wang L, Meng J, Wang S, Geng X, Jia Y, Li M, Yang B, Jenny Lu HA, Zhou H. Inhibiting Focal Adhesion Kinase Ameliorates Cyst Development in Polycystin-1-Deficient Polycystic Kidney Disease in Animal Model. J Am Soc Nephrol. 2021 Sep;32(9):2159-2174. doi: 10.1681/ASN.2020111560.

    合成参考文献


    参考文献:10.1016/j.bmcl.2020.127459
    摘要:Xie H, Lin X, Zhang Y, Tan F, Chi B, Peng Z, Dong W, An D. Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors. Bioorganic & Medicinal Chemistry Letters. 2020 Nov;30(21):127459. doi: 10.1016/j.bmcl.2020.127459.
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