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公开(公告)号:US06710183B2
公开(公告)日:2004-03-23
申请号:US10182109
申请日:2002-07-24
申请人: Janos Fischer , Ildiko Ballo , Endrene Petenyi , Janos Kreidl , Laszlo Czibula , Andras Nemes , Ida Deutschne Juhasz , Eva Werkne Papp , Judit Nagyne Bagdy , Istvan Hegedüs , Jenöme Farkas
发明人: Janos Fischer , Ildiko Ballo , Endrene Petenyi , Janos Kreidl , Laszlo Czibula , Andras Nemes , Ida Deutschne Juhasz , Eva Werkne Papp , Judit Nagyne Bagdy , Istvan Hegedüs , Jenöme Farkas
IPC分类号: C07D25700
CPC分类号: C07D403/10
摘要: A Process is disclosed for preparing a compound of the Formula (I) which comprises the steps of: (a) detritylating a compound of the Formula (III) with 0.1 to 1 equivalent of potassium hydroxide in a C1 to C4 straight chain alcohol solvent to obtain a reaction mixture containing the compound of the Formula (I), (b) changing the C1 to C4 straight chain alcohol solvent in the reaction mixture to an aprotic solvent or a weakly protic solvent, and (c) following step (b) crystallizing out the compound of the Formula (I) from the reaction mixture.
摘要翻译: 公开了制备式(I)化合物的方法,该方法包括以下步骤:(a)在C1至C4直链醇溶剂中用0.1至1当量的氢氧化钾将式(III)的化合物与 得到含有式(I)的化合物的反应混合物,(b)将反应混合物中的C1-C4直链醇溶剂改为非质子溶剂或弱质子性溶剂,和(c)步骤(b) 从反应混合物中除去式(I)的化合物。
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公开(公告)号:US06657062B1
公开(公告)日:2003-12-02
申请号:US09214099
申请日:1998-12-28
申请人: Janos Kreidl , Laszlo Czibula , Andras Nemes , Ida Deutschne Juhasz , Eva Werkne Papp , Juidit Nagyne Bagdy , Laszlo Dobay , Istvan Hegedus , Kalman Harsanyi , Istvan Borza
发明人: Janos Kreidl , Laszlo Czibula , Andras Nemes , Ida Deutschne Juhasz , Eva Werkne Papp , Juidit Nagyne Bagdy , Laszlo Dobay , Istvan Hegedus , Kalman Harsanyi , Istvan Borza
IPC分类号: C07D21118
CPC分类号: C07D405/12 , C07D211/22 , C07D211/70
摘要: A process is disclosed for the preparation of compounds of the formula (I), which compounds are useful as intermediates for the preparation of paroxetine of formula(V).
摘要翻译: 公开了制备式(I)化合物的方法,该化合物可用作制备式(V)的帕罗西汀的中间体。
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公开(公告)号:US20090270630A1
公开(公告)日:2009-10-29
申请号:US12302127
申请日:2007-06-21
申请人: Laszlo Czibula , Ferenc Sebok , Laszlo Dobay , Eva Werkne Papp , Ida Deutschne Juhasz , Judit Nagyne Bagdy , Tamasne Uberhardt
发明人: Laszlo Czibula , Ferenc Sebok , Laszlo Dobay , Eva Werkne Papp , Ida Deutschne Juhasz , Judit Nagyne Bagdy , Tamasne Uberhardt
IPC分类号: C07D417/12
CPC分类号: C07D417/12
摘要: Process for the synthesis of 5-{4-[N-methyl-N-(2-pyridyl)-amino-ethoxy]-benzylidene}-thiazolidine-2,4-dione (INN name: benzylidene-rosiglitazone) of formula (I), which consist of the following steps: Step a) reaction of 2-chloro-pyridine and 2-(N-methylamino)-ethanol Step b) reaction of the obtained compound of formula (III) with 4-fluorobenzaldehyde Step c) reaction of the obtained compound of formula (IV) with thiazolidine-2,4-dione characterized by dissolving 4-{2-[N-methyl-N-(2-pyridyl)amino]-ethanol of formula (III) obtained in Step a) in toluene and using it in Step b) without isolation; reacting the solution of compound of formula (III) in toluene in Step b) with 4-fluorobenzaldehyde in the presence of aqueous alkali hydroxide solution and phase transfer catalyst at 25-50° C.; reacting the solution of the benzaldehyde derivative of formula (IV) obtained in Step b) in toluene in Step c) and isolating the desired product.
摘要翻译: 合成式(I)的5- {4- [N-甲基-N-(2-吡啶基) - 氨基 - 乙氧基] - 亚苄基} - 噻唑烷-2,4-二酮(INN名称:亚苄基 - 罗格列酮) ),其步骤如下:步骤a)2-氯 - 吡啶和2-(N-甲基氨基) - 乙醇的反应步骤b)将所得到的式(III)化合物与4-氟苯甲醛反应步骤c)反应 所得到的式(Ⅳ)化合物与噻唑烷-2,4-二酮的特征在于将步骤a中获得的式(Ⅳ)的4- {2- [N-甲基-N-(2-吡啶基)氨基] - 乙醇 )并在步骤b)中使用它而不分离; 使步骤b)中式(III)化合物在甲苯中的溶液与4-氟苯甲醛在碱金属氢氧化物水溶液和相转移催化剂存在下,在25-50℃下反应。 使步骤b)中获得的式(IV)的苯甲醛衍生物在步骤c)中的甲苯中的溶液反应,并分离所需产物。
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