CAS: 142851-03-4; Ethyl N-Boc-Piperidine-4-Carboxylate

该化合物是有机合成的多用途中间体,特别因其在药用活性化合物的制备中的作用而得到重视.三丁基和乙酯组群提供不同的反应性,允许在温和条件下有选择地取消保护或进一步功能化.该组群在标准储存条件下表现出高度稳定,确保多步合成路线的一贯性.其管里丁基是药用化学中常见的脚架,有利于生物活性分子的发展.双箱里衣功能允许高效的衍生,使研究人员在药物发现和精细化学合成方面有一个实际的选择.

结构式图片

相似化合物

1126-09-6 24228-40-8 24252-37-7

欧盟法规

ECHA物质C&L通报

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合成工艺路线路线简述

    4-哌啶甲酸置于氯化亚砜,三乙胺体系中,用 二氯甲烷 用作溶剂,化学反应 18.0H,反应生成N-Boc-4-哌啶甲酸乙酯
    参考文献:含有哌啶-4-甲酰胺的新型二氮杂螺癸酮衍生物作为几丁质合成酶抑制剂和抗真菌剂的设计,合成和生物学评价
    标题:含有哌啶-4-甲酰胺的新型二氮杂螺癸酮衍生物作为几丁质合成酶抑制剂和抗真菌剂的设计,合成和生物学评价
    摘要:设计,合成了一系列新型2-Oxo-(1-Oxo-2,8-Diazaspiro[4.5]Decane-8-yl)乙基哌啶甲酰胺衍生物,并通过1 H NMR,13 C NMR和hrms光谱对其进行了表征.评估了所有 18 种新制备的化合物对几丁质合成酶 (Chs) 的抑制作用和体外抗真菌活性.酶法分析表明,化合物5H对chs显示出优异的抑制活性,Ic 50值为0.10 Mm,化合物5B,5D和5Q对几丁质合酶显示出非常好的抑制作用,Ic 50值分别为0.13 Mm,0.18 Mm和0.15 Mm,而 Ic 50Ployoxin B 的值为 0.08 Mm.同时,这些化合物中的其他化合物对几丁质合酶表现出中等的抑制效力.抗真菌试验表明,与对照药物氟康唑和多氧菌素 B 相比,化合物5H对这些测试菌株(包括白色念珠菌,烟曲霉,新型念珠菌和黄曲霉)具有优异的抗真菌活性.其优异的抗真菌活性与其优异的几
    Doi:10.1016/j.Bioorg.2021.105108

    海关参考信息

    专利信息


    专利号:WO-2011029896-A1
    优先权日:2009-09-11
    标 题 :Methods of preparation of muscarinic acetylcholine receptor antagonists
    发明人:CARANGIO ANTONELLA; CHEUNG IZABEL; D SOUZA ERIN CARMEN FRANCES; LEAHY JOHN HENRY; STRACHAN JOHN BRYCE
    权利人:GLAXO GROUP LTD; CARANGIO ANTONELLA; CHEUNG IZABEL; D SOUZA ERIN CARMEN FRANCES; LEAHY JOHN HENRY; STRACHAN JOHN BRYCE
    摘要:The present application describes novel intermediates useful in the synthesis of mAChRs and methods for preparing these intermediates, comprising a compound of Formula (II): wherein, P is a suitably nitrogen protecting group; R is selected from the group consisting of C 1 - 8 alkyl, C 2 - 8 alkenyl, C 2 - 8 alkynyl, C 3 - 6 cycloalkyl, C 3 - 6 cycloalkenyl, heterocyclic, heterocyclic C 1 - 4 alkyl, aryl, aryl C 1 - 4 alkyl and heteroaryl C 1 - 4 alkyl; and Y is a suitable leaving group.

    专利号:US-6593347-B2
    优先权日:1998-10-30
    标题 :Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
    发明人:BANDARAGE UPUL K; DONG QING; FANG XINQIN; GARVEY DAVID S; MERCER GREGORY J; RICHARDSON STEWART K; SCHROEDER JOSEPH D; WANG TIANSHENG
    权利人:NITROMED INC
    摘要:The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.

    专利号:WO-2004058727-A1
    优先权日:2002-12-20
    标题 :Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity
    发明人:CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA
    权利人:BAYER PHARMACEUTICALS CORP; CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA
    摘要:This invention relates to substituted 3,5-dihydro-4H-imidazol-4-ones compounds which are useful in the treatment of obesity and obesity-related disorders, and as weight-loss and weight-control agents. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.

    专利号:US-2023010886-A1
    优先权日:2019-09-23
    标 题 :Shp2 inhibitors and uses thereof
    发明人:XIE YINONG; BABISS LEE E
    权利人:SUZHOU PUHE BIOPHARMA CO LTD
    摘要:Compounds of Formula 1 as inhibitors of protein tyrosine phosphatase SHP2 are disclosed. The pharmaceutical compositions comprising compounds of Formula 1, methods of synthesis of these compounds, methods of treatment for diseases associated with the aberrant activity of SHP2 such as cancer using these compounds or compositions containing these compounds are also disclosed.

    专利号:US-2024390383-A1
    优先权日:2021-09-28
    标题 :Dioxazines and their use in treatment of gba-related diseases
    发明人:NEVE SØREN; BROWN WILLIAM DALBY; THIRSTRUP KENNETH
    权利人:ZEVRA DENMARK AS
    摘要:The present invention relates to dioxazines, their synthesis, and their use for increasing GBA activity and/or levels as well as treatment of GBA-related diseases, such as Parkinson's disease.

    专利号:US-2019263782-A1
    优先权日:2005-09-30
    标 题 :Chemical Process for the Synthesis of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline
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    合成参考文献


    摘要:Li, H.; Wang, Y.; Liu, Q., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 539.
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