CAS: 1646839-59-9; N-(5-((6,7-Dimethoxyquinolin-4-yl)Oxy)Pyridin-2-yl)-2,5-Dioxo-1-Phenyl-1,2,5,6,7,8-Hexahydroquinoline-3-Carboxamide

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2,5-二氧代-1-苯基-1,2,5,6,7,8-六氢-3-喹啉羧酸 2,5-Dioxo-1-Phenyl-1,2,5,6,7,8-Hexahydro-3-Quinoline Carboxylic Acid 125885-51-0

合成工艺路线路线简述

    📜2-氯-5-羟基吡啶置于tris(Dibenzylideneacetone)Dipalladium(0) Chloroform Complex,三乙胺,N,N-二异丙基乙胺,Methanaminium,N-[(Dimethylamino)(3H-1,2,3-Triazolo[4,5-B]Pyridin-3-Yloxy)Methylene]-N-Methyl-,Hexafluorophosphate(1-),Lithium Hexamethyldisilazane体系中,用 四氢呋喃,N,N-二甲基甲酰胺,氯苯 用作溶剂,化学反应 157.5H,反应生成N-[5-[(6,7-二甲氧基-4-喹啉基)氧基]-2-吡啶基]-1,2,5,6,7,8-六羟基-2,5-二氧代-1-苯基-3-喹啉甲酰胺
    参考文献:Ethane-Sulfonate Salt Of Quinoline Derivative
    标题:Ethane-Sulfonate Salt Of Quinoline Derivative
    摘要:本发明涉及一种n-{5-[(6,7-二甲氧基-4-喹啉基)氧基]-2-吡啶基}-2,5-二氧杂-1-苯基-1,2,5,6,7,8-六氢-3-喹啉羧酰胺的乙烷磺酸盐,其具有axl抑制活性,并可用作预防和/或治疗免疫性疾病,癌症等的药物,以及其晶体和制药组合物.

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    主要参考文献


    1: Okura N, Nishioka N, Yamada T, Taniguchi H, Tanimura K, Katayama Y, Yoshimura A, Watanabe S, Kikuchi T, Shiotsu S, Kitazaki T, Nishiyama A, Iwasaku M, Kaneko Y, Uchino J, Uehara H, Horinaka M, Sakai T, Tanaka K, Kozaki R, Yano S, Takayama K. ONO-7475, a Novel AXL Inhibitor, Suppresses the Adaptive Resistance to Initial EGFR-TKI Treatment in EGFR-Mutated Non-Small Lung Cancer. Clin Cancer Res. 2020 Jan 17. doi: 10.1158/1078-0432.CCR-19-2321. Epub ahead of print. 102(12):2048-2057. doi: 10.3324/haematol.2017.168856. Epub 2017 Sep 14.

    合成参考文献


    参考文献:10.3324/haematol.2021.278369
    摘要:Post SM, Ma H, Malaney P, Zhang X, Aitken MJL, Mak PY, Ruvolo VR, Yasuhiro T, Kozaki R, Chan LE, Ostermann LB, Konopleva M, Carter BZ, DiNardo C, Andreeff MD, Khoury JD, Ruvolo PP. AXL/MERTK inhibitor ONO-7475 potently synergizes with venetoclax and overcomes venetoclax resistance to kill FLT3-ITD acute myeloid leukemia. haematol. 2021 Nov 04;107(6):1311–22. doi: 10.3324/haematol.2021.278369.
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