Dehydromequitazine置于palladium 10% On Activated Carbon,氢气体系中,用 甲醇 用作溶剂,20.0 °C,101.33 Kpa 条件下,反应 24.0H,以91%的收率获得美喹他嗪 参考文献:Expedient Synthesis Of Mequitazine An Antihistaminic Drug By Palladium Catalyzed Allylic Alkylation Of Sodium Phenothiazinate 标题:Expedient Synthesis Of Mequitazine An Antihistaminic Drug By Palladium Catalyzed Allylic Alkylation Of Sodium Phenothiazinate 摘要:报告了一种简短而直接的抗组胺药物美克替嗪的合成方法,该方法基于在温和条件下,采用钯催化的烯丙基烷基化反应,将1-氮杂双环[2.2.2]辛-2-烯-3-基乙酸甲酯与苯噻嗪钠进行反应. Doi:10.1248/cpb.57.1300
专利号:US-8754074-B2 优先权日:2011-01-10 标题:Vinyl quinuclidine useful as a synthesis intermediate in the preparation of (R)-mequitazine 发明人:NICOLAS MARC; LARQUETOUX LAURENT; LEROUX SÉBASTIEN; DORIS ERIC 权利人:NICOLAS MARC; LARQUETOUX LAURENT; LEROUX SÉBASTIEN; DORIS ERIC; PF MEDICAMENT; COMMISSARIAT ENERGIE ATOMIQUE 摘要:The present invention relates to the use of the vinyl quinuclidine enantiomer (R) of the following formula 2 as a synthesis intermediate in the preparation of (R)-mequitazine.
专利号:US-8304545-B2 优先权日:2007-01-18 标 题:Quinuclidine derivative useful in the preparation of mequitazine 发明人:MIOSKOWSKI CHARLES; GONNOT VANESSA; BAATI RACHID; NICOLAS MARC 权利人:MIOSKOWSKI CHARLES; GONNOT VANESSA; BAATI RACHID; NICOLAS MARC; PF MEDICAMENT 摘要:The invention relates to a 1-aza-bicyclo[2.2.2]oct-2-en-3-ylmethyl acetate of the formula (I), wherein said compound is useful as a synthesis intermediate for the production of mequitazine.
专利号:US-2023271983-A1 优先权日:2020-07-29 标题 :Functionalized isonitriles and products, preparation and uses thereof 发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA 权利人:UNIV SANTIAGO COMPOSTELA 摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.
专利号:EP-1037891-B1 优先权日:1997-12-08 标 题 :Method for preparing mequitazine and novel synthesis intermediate 发明人:GUMINSKI YVES; IMBERT THIERRY; LESIMPLE PATRICK 权利人:PF MEDICAMENT 摘要:The invention concerns a novel method for preparing mequitazine and its laevo-gyrate isomer, consisting in reacting the phenothiazine derivative containing lithium with 3-methane sulphonyl oxymethyl-1-aza-bicyclo(2,2,2)-octane or its laevo-gyrate isomer, in the presence of butyllithium.
专利号:FR-2777278-A1 优先权日:1998-04-09 标 题:NOVEL PROCESS FOR THE PREPARATION OF 3-HYDROXYMETHYL QUINUCLIDINE INTERMEDIATE SYNTHESIS OF MEQUITAZINE
专利号:US-2006153882-A1 优先权日:2001-05-29 标题:Anti-allergic pharmaceutical composition containing at least one allergen and at least on antihistamine compound 发明人:LORIA EMILE; TERRASSE GAETAN; TREHIN YVES 权利人:LORIA EMILE; TERRASSE GAETAN; TREHIN YVES 摘要:The present invention relates to an anti-allergic pharmaceutical composition containing at least two active agents chosen among: (i) one allergen, (ii) one antihistamine compound, (iii) one inhibitor of histamine synthesis, said active agents being associated in said composition with a pharmaceutically acceptable vehicle.
1: Ahn SH, Maeng HJ. Quantification of mequitazine in human plasma by gas chromatography- quadrupole mass spectrometry and its application to a human pharmacokinetic study. Biomed Chromatogr. 2016 Apr;30(4):574-8. doi: 10.1002/bmc.3585. Epub 2015 Sep 20. doi: 10.1021/ol2012567. Epub 2011 Jun 9. doi: 10.1016/j.saa.2009.08.006. Epub 2009 Aug 12. doi: 10.1016/j.talanta.2006.02.059. Epub 2006 May 2. Review. Spanish. Spanish. 9: Kwon OS, Kim HJ, Pyo H, Chung SJ, Chung YB. Determination of mequitazine in human plasma by gas-chromatography/mass spectrometry with ion-trap detector and its pharmacokinetics after oral administration to volunteers. Arch Pharm Res. 2005 Oct;28(10):1190-5. Russian. French. Bulgarian. Japanese.
合成参考文献
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