CAS: 29218-27-7; 5-(Hydroxymethyl)-3-(M-Tolyl)Oxazolidin-2-One

该化合物是一种化学化合物,被归类为单胺氧化酶抑制剂(MAOI),主要用于治疗抑郁,其特点是能够抑制酶单胺氧化酶,因为酶单胺氧化酶是导致脑中...

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5-(Chloromethyl)-3-(M-Tolyl)Oxazolidin-2-One
3-{3-Methylphenyl}-5-(Tetrahydro-2H-2-Pyranyloxy-Methyl)-2-Oxazolidinone 513069-01-7

合成工艺路线路线简述

    📜5-(Iodomethyl)-3-(M-Tolyl)Oxazolidin-2-One置于potassium Acetate,乙醇,Potassium Carbonate体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 13.0H,以75%的收率获得涛洛西酮
    参考文献:通过icl诱导的环化反应,无金属合成恶唑烷-2,4-二酮和3,3-二取代的羟吲哚
    标题:通过icl诱导的环化反应,无金属合成恶唑烷-2,4-二酮和3,3-二取代的羟吲哚
    摘要:本文报道了一种无金属的方法制备恶唑烷-2,4-二酮和羟吲哚.所得产物可用作合成生物活性化合物(例如toloxatone,(+/-)-乙二胺和(+/-)-Phystigtigmine)的关键中间体.
    Doi:10.1002/ejoc.201801250

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    专利信息


    专利号:US-7576211-B2
    优先权日:2004-09-30
    标题 :Synthesis of thienopyridinone compounds and related intermediates
    发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
    权利人:EPIX DELAWARE INC
    摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

    专利号:US-2008214827-A1
    优先权日:2004-02-03
    标 题:Synthesis of Cyanoimino-Benzoimidazoles
    发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
    权利人:EURO CELTIQUE SA
    摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

    专利号:US-7309799-B2
    优先权日:2004-06-01
    标 题:Methods for the synthesis of milnacipran and congeners thereof
    发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V
    权利人:COLLEGIUM PHARMACEUTICAL INC
    摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

    专利号:US-7354923-B2
    优先权日:2001-08-10
    标 题 :Piperazine melanocortin-specific compounds
    发明人:SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH
    权利人:PALATIN TECHNOLOGIES INC
    摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure: n nand stereoisomer and pharmaceutically acceptable salts thereof, where X is CH 2 or Câ•?O, R 1 , R 2 , and R 3 are as described in the specification, preferably where R 3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R 3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.

    专利号:US-2005282898-A1
    优先权日:2004-06-01
    标 题 :Methods for the synthesis of milnacipran and congeners thereof

    专利号:US-2006084805-A1
    优先权日:2004-09-30
    标题:Synthesis of thienopyridinone compounds and related intermediates

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Baek SC, Kang MG, Park JE, Lee JP, Lee H, Ryu HW, Park CM, Park D, Cho ML, Oh SR, Kim H. Osthenol, a prenylated coumarin, as a monoamine oxidase A inhibitor with high selectivity. Bioorg Med Chem Lett. 2019 Mar 15;29(6):839-843. doi: 10.1016/j.bmcl.2019.01.016. Epub 2019 Jan 18. doi: 10.1016/j.bioorg.2018.10.051. Epub 2018 Oct 28. doi: 10.1016/j.bmcl.2018.06.023. Epub 2018 Jun 18. doi: 10.1016/j.jsps.2018.02.012. Epub 2018 Feb 6.
    5: Erol Gunal S, Teke Tuncel S, Gokhan Kelekci N, Ucar G, Yuce Dursun B, Sag Erdem S, Dogan I. Asymmetric synthesis, molecular modeling and biological evaluation of 5-methyl-3-aryloxazolidine-2,4-dione enantiomers as monoamine oxidase (MAO) inhibitors. Bioorg Chem. 2018 Apr;77:608-618. doi: 10.1016/j.bioorg.2018.02.003. Epub 2018 Feb 10. doi: 10.1016/j.bmcl.2018.01.049. Epub 2018 Jan 31. doi: 10.1016/j.ejps.2018.01.013. Epub 2018 Jan 8. doi: 10.1016/j.ijbiomac.2017.01.080. Epub 2017 Jan 18. doi: 10.1016/j.ejmech.2016.09.007. Epub 2016 Sep 4. doi: 10.1016/j.ejmech.2015.10.025. Epub 2015 Oct 23. Review. doi: 10.1016/j.ejps.2015.02.006. Epub 2015 Feb 17. doi: 10.1002/dta.1530. Epub 2013 Sep 20. doi: 10.1016/j.ab.2009.10.029. Epub 2009 Oct 20. Review.

    合成参考文献


    摘要:Drugs of the Future., 1(569), 1976
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