CAS: 695-37-4; 3-Fluoropyridine 1-Oxide

该化合物是一种氟化的环环化合物,其核心为原子和N-氧化功能组,以氟原子和N-氧化功能组替代.这种结构具有独特的反应性,在制药和农用化学合成中作为多功能中间体具有价值.氟和N-氧化组的电子抽取效应增强了其在核生殖替代和交叉反应中的效用.在各种反应条件下,这种化合物的稳定性允许精确的功能化,而极地N-氧化物会提高极地溶剂的溶解性.该化合物在开发氟化生物活性分子方面特别有用,因为其独特的电子特性可以影响代谢稳定性和结合性.

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CAS号372-47-4 3-氟吡啶 | CAS号372-47-4 3-氟吡啶 | CAS号97509-75-6 2-氰基-3-氟吡啶 | CAS号2247-88-3 4-氨基-3-氟吡啶 | CAS号769-54-0 3-氟-4-硝基-N-氧化吡啶 | CAS号70682-09-6 2-氯吡啶-3-磺酰氯

合成工艺路线路线简述

    📜3-氟吡啶置于间氯过氧苯甲酸体系中,用 二氯甲烷 作为反应溶剂,以21%的收率获得产物3-氟吡啶 N-氧化物
    参考文献:金催化中氮氧化物的策略性方法-一个案例研究
    标题:金催化中氮氧化物的策略性方法-一个案例研究
    摘要:对(氧化)金催化的选定关键反应的广泛动力学研究集中在催化活性的降低,这是由于吡啶衍生物引起的金(i)催化剂的抑制,如果使用n氧化物作为副产物获得的吡啶衍生物氧气供体.不管它们的市售性如何,都已对受检吡啶衍生物及其相应的n-氧化物进行了选择.特别注意的是迄今为止在大多数反应筛选中都被忽略的实际益处.用gc和1监测测试反应1 H NMR光谱.所接收的反应常数提供了关于杂环的电子结构与催化活性之间的相关性的信息.根据收集的动力学数据,有可能开发出一套基本的三种n氧化物,这些氧化物必须在进一步的氧化金(i)催化反应中加以考虑.
    DOI:10.1002/adsc.201801007

    海关参考信息

    专利信息


    专利号:US-2017355648-A1
    优先权日:2016-04-26
    标题 :Synthesis of meta-substituted [18f]-3-fluoro-4-aminopyridines by direct radiofluorination of pyridine n-oxides

    专利号:US-10160695-B2
    优先权日:2016-04-26
    标 题 :Synthesis of meta-substituted [18F]-3-fluoro-4-aminopyridines by direct radiofluorination of pyridine N-oxides
    发明人:BRUGAROLAS PEDRO
    权利人:UNIV CHICAGO
    摘要:Disclosed herein are methods for the fluorination aromatic N-heterocyclic N-oxides that comprise at least one leaving group. The N-oxides may be reduced to the fluorinated aromatic N-heterocyclic amine analogs. This novel fluorination approach may be successfully applied for synthesizing aromatic N-heterocyclic compounds labeled with 18 F.

    专利号:US-10738028-B2
    优先权日:2016-05-11
    标题:Spiro three-membered ring, spiro five-membered ring peptide deformylase inhibitor and use thereof in antibacteria and anti-tumor
    发明人:HU WENHAO; LV FENGPING; TANG YANG; LI ZIYAN; CHEN CHEN; WEI JIANHAI; DONG SUZHEN; QIAN YU
    权利人:RUDONG RUIEN PHARMACEUTICAL TECH CO LTD
    摘要:Disclosed are the anti-bacterial activity and the anti-tumor activity of a class of new spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, are effective against many antibiotic-resistant Gram-positive strains by inhibiting the activity of the peptide deformylase required in the synthesis of bacterial proteins, and do not affect the synthetic process of the main proteins of the human body, thus selectively killing bacteria. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, can affect the energy balance of the cancer cells through inhibiting the peptide deformylase of the mitochondria in the cells, so that the mitochondrial membrane is depolarized, ATP is exhausted and cell apoptosis is promoted, and has good inhibitory activities on many cancer cell strains such as colorectal cancer, leukemia, lung cancer, gastric cancer, cervical cancer, breast cancer, prostatic cancer, liver cancer and osteosarcoma at relatively lower concentrations. The structure of exemplary invention spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitors are represented by one or more of:

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    ✅ COA系统入驻 | 共享模式

    合成参考文献


    摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 267.
    摘要:Jiao, N.; Li, Z., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 703.
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