CAS: 455-15-2; 4-Fluorophenyl Methyl Sulfone

该化合物是一种氟化磺化合物,其特点是其稳定的磺酰氟功能组和芳烃氟化烃替代物,这种结构具有独特的再活性,使其成为有机合成中有价值的中间体,特别是在制药和农用化学应用中.氟原子会增强电子提取特性,影响该化合物的紧凑性,活性成分的代谢稳定性.其高纯度和定义明确的化学特性确保了交叉反应,核细胞替代和其他变异的一致性能.该化合物通常作为白色晶状固体供应,在普通有机溶剂中具有良好的溶解性,便于在实验室和工业环境中的处理.在标准条件下,其稳定性进一步支持其在多步骤合成途径中的实用性.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

fluorobenzene p-fluorothioanisole methanesulfonyl chloride 4-fluorophenyl methyl sulfoxide 1-fluoro-4-methanesulfonyl-2-nitrobenzene 4-(4'-methylphenyloxy)-phenyl methyl sulfone

合成工艺路线路线简述

    4-甲基磺酰苯酚置于1,8-二氮杂双环[5.4.0]十一碳-7-烯,1,3-Bis(2,6-Diisopropylphenyl)-2-Chloroimidazolium Dihydrogen Trifluoride体系中,用 甲苯 作为反应溶剂,以84 %的收率获得产物对氟苯甲砜
    参考文献:缺电子酚的脱氧氟化
    标题:缺电子酚的脱氧氟化
    摘要:在这项研究中,我们报告了在环境条件下使用次氯酸盐作为氯化剂在水性介质中轻松合成 2-Chloro-1,3-Bis(2,6-Diisopropylphenyl)Imidazolium 盐.此外,还提出了一种基于聚[氟化氢]盐的空气稳定且对水分不敏感的脱氧氟化试剂,它能够在 Dbu 作为碱存在下将缺电子酚或芳基甲硅烷基醚转化为相应的芳基氟化物,具有非常好的产量和对官能团的高耐受性.
    DOI:10.1021/acs.Orglett.3C01018

    海关参考信息

    专利信息


    专利号:US-2005119332-A1
    优先权日:1998-03-12
    标 题 :Substituted thiophene compounds as modulators of protein tyrosine phosphatases (PTPases)
    发明人:JEPPESEN LONE; ANDERSEN HENRIK S; OLSEN OLE H; JUDGE LUKE M; HOLSWORTH DANIEL D; BAKIR FARID; AXE FRANK U; GE YU
    摘要:The present invention provides novel compounds of formula 1a, n nnovel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.

    专利号:US-2002165398-A1
    优先权日:1998-03-12
    标题:Modulators of protein tyrosine phosphatases (PTPases)
    发明人:JEPPESEN LONE; ANDERSEN HENRIK SUNE; OLSEN OLE HVILSTED; JUDGE LUKE MILBURN; HOLSWORTH DANIEL DALE; BAKIR FARID; AXE FRANK URBAN; GE YU
    摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. n The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimers disease and schizophrenia, and infectious diseases.

    专利号:US-4554381-A
    优先权日:1982-01-21
    标题:Process for sulfonylation of halobenzenes
    发明人:DESBOIS MICHEL
    权利人:RHONE POULENC SPEC CHIM
    摘要:A process for sulfonylation of halobenzenes, in which a halobenzene is reacted with a sulfonic acid, a precursor or a derivative thereof in the presence of boron trifluoride in an amount such that the absolute pressure of boron trifluoride within the reaction vessel exceeds 1 bar, and in the presence of hydrofluoric acid as a solvent. The resultant products are useful as intermediates in the synthesis of compounds having a phytosanitary (e.g., herbicidal) or pharmaceutical activity.

    专利号:US-2002128496-A1
    优先权日:2001-01-12
    标题 :Process for the preparation of matrix metalloproteinase inhibitors
    发明人:CHANG SOU-JENG; FERNANDO DILINIE P; GUPTA ASHOK; HILL DAVID R; WITTENBERGER STEVEN J
    摘要:The present invention discloses a process for the synthesis of reverse hydroxamate matrix metalloproteinase (MMP) inhibitors.

    专利号:US-2022401561-A1
    优先权日:2019-09-30
    标题 :Protein-macromolecule conjugates and methods of use thereof
    发明人:SONG YUNTAO; LI HUI; ZHOU HAIPING; LIAO CHUAN
    权利人:BEIJING XUANYI PHARMASCIENCES CO LTD
    摘要:The present disclosure provides protein-macromolecule conjugates, releasable linkers, and macromolecules, as defined herein. The disclosed conjugates provide unique properties that ae based at least upon the properties of linker and number of linker-Macromolecule moieties. Also provided herein are a method of synthesis and use of conjugates in treating diseases and disorders.

    专利号:EP-1383735-A4
    优先权日:2001-05-02
    标题 :PROCESSES FOR THE SYNTHESIS OF ACYLANILIDES COMPRISING BICALUTAMIDE AND DERIVATIVES THEREOF
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    主要参考文献

    [参考文献]: Carol K Wada, Et Al. Phenoxyphenyl Sulfone N-Formylhydroxylamines (Retrohydroxamates) As Potent, Selective, Orally Bioavailable Matrix Metalloproteinase Inhibitors. J Med Chem. 2002 Jan 3;45(1):219-32.

    合成参考文献


    摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 984.
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