CAS: 78162-58-0; N,N-Dimethyl-1H-Imidazole-1-Sulfonamide

该化合物是一种具有有机合成和制药研究应用的硫基可功能化非碘化衍生物,其关键结构特征--二甲基硫磺酰基组--作为硫代基剂的增生活性,能够有选择地改变核嗜血基质;化合物在标准条件下表现出稳定性,便于处理和储存;其二硝基甲酰基在热循环化学中促进多功能性,在生物活性分子的开发中起到先质或中间作用;电镀硫磺酰胺协会进一步提高其在交叉相交和功能组变中的效用;该试剂因其在引入硫代基组方面的效率而特别受重视,因此成为药用化学和材料科学应用的实用选择.

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合成工艺路线路线简述

    2-[二甲基(2-甲基-2-丙基)甲硅烷基]-N,N-二甲基-1H-咪唑-1-磺酰胺置于四丁基氟化铵体系中,用 四氢呋喃 作为反应溶剂,化学反应 0.5H,反应生成 N,N-二甲基咪唑-1-磺酰胺
    参考文献:Ngochindo,Raphael I.,Journal Of The Chemical Society. Perkin Transactions I,1990,# 6,P. 1645-1648
    标题:Ngochindo,Raphael I.,Journal Of The Chemical Society. Perkin Transactions I,1990,# 6,P. 1645-1648

    海关参考信息

    专利信息


    专利号:US-5359051-A
    优先权日:1990-01-11
    标题 :Compounds useful in the synthesis of nucleic acids capable of cleaning RNA
    发明人:COOK PHILLIP D; GUINOSSO CHARLES J; BRUICE THOMAS
    权利人:ISIS PHARMACEUTICALS INC
    摘要:Compositions and methods for modulating the activity of RNA are disclosed. In accordance with preferred embodiments, antisense compositions are prepared comprising targeting and reactive portions. In preferred embodiments, the reactive portions comprise one or two imidazole functionalities conjugated to the targeting oligonucleotide via linkers with and without intervening intercalating moieties and act through phosphorodiester hydrolytic bond cleavage. Therapeutics, diagnostics and research methods are also disclosed. Synthetic nucleosides and nucleoside fragments are also provided which are useful for elaboration of oligonucleotides for such purposes.

    专利号:US-2009118512-A1
    优先权日:2006-03-31
    标 题:Process for Preparing 6,7-Dihydro-5H-Imidazo[1,5-A]Pyridin-8-One
    发明人:MARTIN PIERRE; BOUDIER ANDREAS; QUIRMBACH MICHAEL; MAH ROBERT; JOTTERAND NATHALIE
    权利人:MARTIN PIERRE; BOUDIER ANDREAS; QUIRMBACH MICHAEL; MAH ROBERT; JOTTERAND NATHALIE
    摘要:6,7-Dihydro-5H-imidazo[1,5-a]pyridin-8-one (I), is obtainable in high yields by: 1) a process which proceeds from a suitably protected C-(3-hydroxypyridin-2-yl)methylamine whose amine is converted to the formamide which is then cyclized to the imidazo[1,5-a]pyridine and hydrogenated to the 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one, and suitably protected C-(3-hydroxypyridin-2-yl)methylamines can be prepared either in 2 steps proceeding from commercially available 3-hydroxy-2-cyanopyridine [932-35-4] or in 3 steps proceeding from commercially available 2-hydroxymethylpyridin-3-ol [14173-30-9]; 2) a process for preparing 4-hydroxy-1-(1H-imidazol-4-yl)butan-1-one, an intermediate from the synthesis of 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one (formula I), as described in WO 2002/040484, proceeding from N,N-dimethyl-2-(trialkylsilanyl)imidazole-1-sulphonamide by lithiation and subsequent reaction with a suitably protected 4-hydroxybutyraldehyde, followed by oxidation of the secondary alcohol, acid-induced deprotection of the imidazole and deprotection of the alcohol functionality; 3) a process which proceeds from 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine [38666-30-7], which is oxidized.

    专利号:WO-9506037-A1
    优先权日:1993-08-27
    标题 :New imidazole derivatives having agonistic or antagonistic activity on the histamine h3 receptor
    发明人:VOLLINGA ROELANT CHRISTIAAN; MENGE WIRO MICHAEL PETRUS BERN; TIMMERMAN HENDRIK
    权利人:VRIJE UNIVERSITEIT; VOLLINGA ROELANT CHRISTIAAN; MENGE WIRO MICHAEL PETRUS BERN; TIMMERMAN HENDRIK
    摘要:The invention relates to new imidazole derivatives of formula (I) having agonistic and antagonistic activity on the histamine H3-receptor. More in particular the invention concerns 4- and 5-substituted aminoalkyl imidazoles and their derivatives. The invention further relates to the synthesis of these compounds, pharmaceutical compositions comprising the said compounds or pharmacological salts thereof, and the use of the compounds as agents having biological activity on the histamine H3-receptor or for the preparation of a pharmaceutical composition.

    专利号:CN-104507928-A
    优先权日:2012-07-03
    标 题:Heterocyclic regulators of lipid synthesis

    专利号:KR-20160100329-A
    优先权日:2013-12-20
    标题 :Heterocyclic modulators of lipid synthesis and combinations thereof

    专利号:CN-106061963-A
    优先权日:2013-12-20
    标题 :Heterocyclic modulators of lipid synthesis and combinations thereof
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    合成参考文献


    摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2004).
    摘要:Gribble, G. W., Science of Synthesis, (2006) 8, 381.
    摘要:Grimmett, M. R., Science of Synthesis, (2002) 12, 492.
    摘要:Grimmett, M. R., Science of Synthesis, (2002) 12, 474.
    摘要:Grimmett, M. R., Science of Synthesis, (2002) 12, 480.
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