CAS: 148-65-2; N'-[(5-Chlorothiophen-2-yl)Methyl]-N,N-Dimethyl-N'-Pyridin-2-Ylethane-1,2-Diamine

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2-chloropyridine 2-Chloro-5-(chloromethyl)thiophene N,N-dimethyl-N'-(pyridine-2-yl)ethane-1,2-diamine 2-aminopyridine

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    📜2-氯-5-氯甲基噻吩置于2,6-二甲基吡啶体系中,化学反应生成氯吡林
    参考文献:抗组胺药;取代的n,N-二甲基-N'-(2-吡啶基)-N'-乙烯基乙二胺作为抗组胺剂.
    标题:抗组胺药;取代的n,N-二甲基-N'-(2-吡啶基)-N'-乙烯基乙二胺作为抗组胺剂.
    摘要:
    Doi:10.1021/jo01154A005

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    专利信息


    专利号:WO-9837078-A1
    优先权日:1997-02-20
    标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
    发明人:DOERWALD FLORENCIO ZARAGOZA
    权利人:NOVO NORDISK AS
    摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

    专利号:US-6136984-A
    优先权日:1996-04-22
    标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
    发明人:DOERWALD FLORENCIO ZARAGOZA
    权利人:NOVO NORDISK AS
    摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

    专利号:WO-9740034-A1
    优先权日:1996-04-22
    标题:Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes

    专利号:EP-1021435-A1
    优先权日:1996-04-22
    标题:Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes

    专利号:CN-101418028-A
    优先权日:2003-06-30
    标题:Synthesis of β-L-2'-deoxynucleoside

    专利号:CA-1188323-A
    优先权日:1981-02-26
    标 题 :3-phenoxybenzyl compounds, production thereof and use thereof for the synthesis of biocides

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Bronchoconstrictor and bronchodilator actions of antihistamine drugs D. F. Hawkins Br J Pharmacol Chemother. 1955 Jun; 10(2): 230–239. doi: 10.1111/j.1476-5381.1955.tb00088.x 1952 Nov 22; 2(4794): 1146–1147. PMCID: PMC2021897

    合成参考文献


    摘要:Gosselin, R.E., R.P. Smith, H.C. Hodge. Clinical Toxicology of Commercial Products. 5th ed. Baltimore: Williams and Wilkins, 1984., p. II-378
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