CAS: 2795-41-7; 6-Fluoro-1H-Indole-3-Carbaldehyde

该化合物是一种氟化的单极衍生物,在有机合成和制药研究方面非常有用;在6个位置上存在氟原子,这增强了它的活性和选择性,使其成为建造复杂的异环化合物的宝贵中间体;在3个位置上,甲醛功能组允许进一步衍生,有利于在药用化学中应用,特别是在生物活性分子的开发中应用;其明确界定的结构和高纯度确保交叉反应,凝聚和其他变异的一致性能;该化合物在合成基于无粉的药品的氟类似物方面特别有用,提供了更好的代谢稳定性和药物发现努力的结合.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

6-氟吲哚 6-Fluoro-1H-Indole 399-51-9

合成工艺路线路线简述

    N,N-Dimethyl-2-(4-Fluoro-2-Nitrophenyl)Ethenylamine置于sodium Hydroxide,镍,肼,三氯氧磷体系中,用 甲醇 用作溶剂,化学反应生成6-氟吲哚-3-甲醛
    参考文献:Novel Tryptophan Dioxygenase Inhibitors And Combined Tryptophan Dioxygenase/5-Ht Reuptake Inhibitors
    标题:Novel Tryptophan Dioxygenase Inhibitors And Combined Tryptophan Dioxygenase/5-Ht Reuptake Inhibitors
    摘要:Tryptophan Dioxygenase (Tdo) Is A Liver Enzyme That Is Responsible For The Majority Of The Metabolism Of Tryptophan. A Series Of Novel 3-(2-Pyridylethenyl)Indoles Are Shown To Be Potent Inhibitors Of Tdo With Selected Members Of The Series Also Having 5-Hydroxy Tryptamine (5-Ht) Reuptake Inhibitory Activity. These Compounds Are Shown To Provide Significant Increases In The Levels Of Tryptophan And 5-Ht In The Cerebrospinal Fluid And Are Thus Of Interest For Antidepressant Therapy. Copyright (C) 1996 Elsevier Science Ltd
    Doi:10.1016/0960-894X(96)00124-2

    海关参考信息

    专利信息


    专利号:US-2008242662-A1
    优先权日:2005-05-31
    标题 :Organic Compounds
    发明人:NIHONYANAGI ATSUKO; TOYAO ATSUSHI; IWAKI YUKI; MASUYA KEIICHI
    权利人:NIHONYANAGI ATSUKO; TOYAO ATSUSHI; IWAKI YUKI; MASUYA KEIICHI
    摘要:The invention relates to substituted 3,4- or higher substituted piperazine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds are especially of the formula I, n n n n n n n n n n wherein R1, R2, R11, C, E and D are as defined in the specification.

    专利号:US-8178559-B2
    优先权日:2004-12-30
    标 题:Organic compounds
    发明人:BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI
    权利人:BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI; NOVARTIS AG
    摘要:3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.
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    合成参考文献


    摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2017) 1, 303.
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