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1. 发明公开

KR1020060121768A 테트라플루오로벤질 아닐린 유도체 및 이의 약학적으로허용가능한 염 화합물의 제조방법 无效
标题翻译：取代的四氢呋喃并嘧啶化合物的制备方法及其药物批准的盐
公开(公告)号：KR1020060121768A
公开(公告)日：2006-11-29
申请号：KR1020060047284
申请日：2006-05-25
申请人： 제이더블유중외제약 주식회사
发明人： 황태섭 , 김현규
IPC分类号： C07C213/02
CPC分类号： C07C227/04 , C07C229/64 , C07C251/24
摘要： Provided is a method for preparing substituted tetrafluorobenzylaniline derivatives and pharmaceutically acceptable salts thereof, which inhibits the formation of dimer impurities and provides tetrafluorobenzylaniline derivatives having storage stability and reduced toxicity. The method for preparing a substituted tetrafluorobenzylaniline compound represented by the following formula I and pharmaceutically acceptable salts thereof comprises the steps of: subjecting tetrafluorobenzyl alcohol to an oxidation reaction to prepare tetrafluorobenzaldehyde; subjecting the prepared tetrafluorobenzaldehyde and 5-amino-salicylic acid to dehydration condensation to prepare a tetrafluorobenziridine-5-aminosalicylic acid compound represented by the following formula II; and subjecting the tetrafluorobenziridine-5-aminosalicylic acid compound to hydrogenation.
摘要翻译：提供了制备取代的四氟苄苯胺衍生物及其药学上可接受的盐的方法，其抑制二聚体杂质的形成，并提供具有储存稳定性和降低的毒性的四氟苄基苯胺衍生物。由下式I表示的取代的四氟苄基苯胺化合物及其药学上可接受的盐的制备方法包括以下步骤：使四氟苄醇进行氧化反应以制备四氟苯甲醛; 将所制备的四氟苯甲醛和5-氨基水杨酸进行脱水缩合，制备由下式II表示的四氟苯并吡啶-5-氨基水杨酸化合物; 并使四氟苯并吡啶-5-氨基水杨酸化合物氢化。

2. 发明公开

KR1020030040858A 심바스타틴의 신규 제조방법 无效
标题翻译：辛伐他汀的制备
公开(公告)号：KR1020030040858A
公开(公告)日：2003-05-23
申请号：KR1020010071445
申请日：2001-11-16
申请人： 제이더블유중외제약 주식회사
发明人： 강성호 , 김종민 , 황태섭 , 김현규
IPC分类号： C07D309/30
摘要： PURPOSE: Provided is a preparation method of simvastatin, which has excellent inhibition activity of HMG-CoA reductase and is thus useful as a therapeutic agent for Hyperlipemia, in high yields. CONSTITUTION: A preparation method of simvastatin comprises the steps of: preparing diol lactone of the formula(III) by deacylation of a lovastatin of the formula(II) in the presence of phase transfer catalyst then followed by heat-refluxing; reacting secondary alcohol at pyranone ring of diol lactone with 2,3-dihydro-2H-pyrane in the presence of acid-catalyst to prepare 4-THP-diol lactone of the formula(IV) containing a tetrahydropyranyl group; coupling 4-THP-diol lactone with 2,2-dimethylbutylchloride to prepare 4-THP-simvastatin of the formula(V); and removing the tetrahydropyranyl group from 4-THP-simvastatin in the presence of acid catalyst.
摘要翻译：目的：提供辛伐他汀的制备方法，其具有优异的HMG-CoA还原酶抑制活性，因此可用作高脂血症的治疗剂。构成：辛伐他汀的制备方法包括以下步骤：在相转移催化剂存在下，通过使式（II）的洛伐他汀脱酰化然后加热回流来制备式（III）的二醇内酯; 在酸催化剂存在下，使二醇内酯的吡喃酮与二氢-2H-吡喃的仲醇反应制备含有四氢吡喃基的式（Ⅳ）的4-THP-二醇内酯; 将4-THP-二醇内酯与2,2-二甲基丁基氯反应制备式（V）的4-THP-辛伐他汀; 并在酸催化剂存在下从4-THP-辛伐他汀中除去四氢吡喃基。

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