칸데사르탄실렉세틸의 개선된 제조방법
    4.
    发明公开
    칸데사르탄실렉세틸의 개선된 제조방법 失效
    改进CANDESARTAN CILEXETIL的方法

    公开(公告)号:KR1020120067819A

    公开(公告)日:2012-06-26

    申请号:KR1020100129430

    申请日:2010-12-16

    CPC classification number: Y02P20/55 C07D403/10 A61K31/4184

    Abstract: PURPOSE: An improved method for preparing candesartan cilexetil is provided to simplify entire process under a mild condition. CONSTITUTION: A method for preparing candesartan cilexetil of chemical formula 1 comprises: a step of dissolving a compound of chemical formula 2 in a dichloromethane solution; a step of adding a mixture solution of alcohol and acetyl chloride to the dichloromethane solution; a step of deprotecting to remove triphenyl methane protection groups and obtain a compound of chemical formula 1; a step of adding ethyl acetate and n-hexane and precipitating the compound of chemical formula 1.

    Abstract translation: 目的:提供一种改进的坎地沙坦替卡西汀的制备方法,以简化温和条件下的整个过程。 构成:制备化学式1的坎地沙坦酯的方法包括:将化学式2的化合物溶解在二氯甲烷溶液中的步骤; 将醇和乙酰氯的混合溶液加入到二氯甲烷溶液中的步骤; 去除三氯甲烷保护基并脱除化学式1化合物的步骤; 加入乙酸乙酯和正己烷并使化学式1的化合物沉淀的步骤。

    레바미피드의 제조방법
    5.
    发明公开
    레바미피드의 제조방법 失效
    制备复方制剂的方法

    公开(公告)号:KR1020030050412A

    公开(公告)日:2003-06-25

    申请号:KR1020010080842

    申请日:2001-12-18

    Abstract: PURPOSE: A process for preparing rebamipide is provided, thereby simplifying the preparing process of rebamipide and improving the preparation yield of rebamipide. CONSTITUTION: A process for preparing rebamipide of the formula(1) comprises the steps of: reacting 4-(bromomethyl)-1,2-dihydro-2-quinolinone of formula(2) with diethyl 2-£(4-chlorobenzoyl)amino|malonate of formula(3) to prepare a compound of formula(4); and reacting the compound of formula(4) under basic conditions, wherein R is alkyl having the carbon number of 1 to 6, wherein the diethyl 2-£(4-chlorobenzoyl)amino|malonate of formula(3) is prepared by reacting diethyl 2-aminomalonate hydrochloride with 4-chlorobenzoyl derivative of formula(6); and R is alkyl having the carbon number of 1 to 6 and X is OH or halogen atom.

    Abstract translation: 目的:提供制备瑞巴派特的方法,从而简化了雷巴米特的制备过程,提高了瑞巴派特的制备成品率。 构成:制备式(1)的瑞巴派特的方法包括以下步骤:使式(2)的4-(溴甲基)-1,2-二氢-2-喹啉酮与2-(4-氯苯甲酰基)氨基 (3)的丙二酸酯以制备式(4)的化合物; 并在碱性条件下使式(4)的化合物反应,其中R是碳数为1至6的烷基,其中式(3)的2-(2-氯苯甲酰基)氨基丙二酸二乙酯是通过使二 2-氨基马来酸盐酸盐与式(6)的4-氯苯甲酰基衍生物反应; R为碳原子数1〜6的烷基,X为OH或卤素原子。

    신규 퀴놀론 카르복실산 유도체
    6.
    发明公开
    신규 퀴놀론 카르복실산 유도체 无效
    新的喹诺酮羧酸衍生物

    公开(公告)号:KR1019990024314A

    公开(公告)日:1999-04-06

    申请号:KR1019970040811

    申请日:1997-08-26

    Abstract: 본 발명은 AIDS(Acquired Immunodeficiency Syndrome)를 유발하는 HIV(Human Immunodeficiency Virus)의 증식에 필수효소인 역전사효소를 저해하는 작용이 우수한 신규 퀴놀론 카르복실산 유도체에 관한 것으로서, 더욱 상세하기로는 다음 화학식 1로 표시되는 퀴놀론 카르복실산 유도체, 그의 약제학적으로 허용가능한 염 및 그의 제조방법에 관한 것이다.

    상기 화학식에서
    X는 CH 또는 질소원자이고, A 는 3-아미노피롤리딘, C
    1-3 의 저급알킬기가 1-3개 치환 또는 비치환된 피페라진이고, B 는 1-나프틸 또는 2-나프틸기이다.

    개선된 자보플록사신의 제조방법
    7.
    发明公开
    개선된 자보플록사신의 제조방법 审中-实审
    ZABOFLOXACIN的改进制造方法

    公开(公告)号:KR1020150133433A

    公开(公告)日:2015-11-30

    申请号:KR1020140060112

    申请日:2014-05-20

    CPC classification number: C07D471/04 C07D487/10

    Abstract: 본발명은자보플록사신 D-아스파르트산염의개선된제조방법에관한것이다. 본발명은자보플록사신 D-아스파르트산염을제조하기위하여사용하는출발물질인 8-메톡시이미노-2,6-디아자-스피로[3,4]옥탄-2-카르복실산 t-부틸에스테르숙신산염(TBDCS) 또는 2-(2,2,2-트리플루오로-아세틸)-2,6-디아자-스피로[3.4]옥탄-8-온-메틸옥심메탄설폰산염(TDMOS)의신규한제조방법을제공한다. 본발명에따른제조방법은상기출발물질을높은수율과높은품질(HPLC 순도; 99.5% 이상)로제조할수 있어, 대량생산에적합하며, 치환반응시 TBDCS나 TDMOS를 1.0~1.1 당량을사용하여획기적으로생산단가를절감할수 방법을제공하기때문에자보플록사신 D-아스파르트산염의대량생산에유용하게이용될수 있다.

    Abstract translation: 本发明涉及一种制造扎布沙星D-天冬氨酸盐的改进方法。 本发明提供了制备用于制备扎布沙星D-天冬氨酸盐,8-甲氧基亚氨基-2,6-二氮杂 - 螺[3,4]辛烷-2-甲酸叔丁酯琥珀酸酯的引发剂的新方法 酸性盐(TBDCS)或2-(2,2,2-三氟 - 乙酰基)-2,6-二氮杂 - 螺[3,4]辛烷-8-对O-甲基肟甲磺酸盐(TDMOS)。 根据本发明的制造方法可以以高产率和质量(HPLC纯度;高于99.5%)制造引发剂,从而适合批量生产。 另外,该方法提供了在取代反应的情况下使用1.0〜1.1当量的TBDCS或者TDMOS来显着降低生产成本的方法,从而有效地用于批量生产扎布沙星D-天冬氨酸盐。

    텔미사탄의 개선된 제조방법
    8.
    发明公开
    텔미사탄의 개선된 제조방법 无效
    改进TELMISARTAN的改进方法

    公开(公告)号:KR1020110094751A

    公开(公告)日:2011-08-24

    申请号:KR1020100014346

    申请日:2010-02-17

    CPC classification number: C07D403/04

    Abstract: PURPOSE: A method for preparing telmisartan is provided to easily remove inorganic salt using a reaction solvent and to simplify reaction process without a separate process. CONSTITUTION: A method for preparing telmisartan of chemical formula 1 comprises: a step of condensing a compound of chemical formula 2 and a compound of chemical formula 3 using dimethyl sulfoxide and isopropanol to prepare a compound of chemical formula 4; and a step of hydrolyzing the compound of chemical formula 4 in a mixture solvent of methanol and purified water.

    Abstract translation: 目的:提供替米沙坦制备方法,以便使用反应溶剂轻松除去无机盐,并简化反应过程,无需单独的工艺。 构成:化学式1的替米沙坦的制备方法包括:使用二甲基亚砜和异丙醇将化学式2的化合物与化学式3的化合物缩合以制备化学式4的化合物的步骤; 以及在甲醇和净化水的混合溶剂中水解化学式4的化合物的步骤。

    2-시아노-3-히드록시-엔-[(4-트리플루오로메틸)페닐]부트-2-엔아미드의 제조방법
    9.
    发明公开
    2-시아노-3-히드록시-엔-[(4-트리플루오로메틸)페닐]부트-2-엔아미드의 제조방법 无效
    制备2-氰基-3-羟基-N - [(4-三氟甲基)苯基] -2-ENAMIDE的方法

    公开(公告)号:KR1020110054670A

    公开(公告)日:2011-05-25

    申请号:KR1020090111413

    申请日:2009-11-18

    Abstract: PURPOSE: A process for preparing 2-cyano-3-hydroxy-N-[(4-trifluoromethyl)phenyl]but-2-enamide is provided to easily remove by-products generated during the manufacturing process of final products. CONSTITUTION: A process for preparing 2-cyano-3-hydroxy-N-[(4-trifluoromethyl)phenyl]but-2-enamide of chemical formula 1 from a compound of chemical formula 5 comprises the steps of: activating a compound of chemical formula 2 to an esterified compound using a carbodiimide compound; and reacting the resultant with a compound of chemical formula 4 to prepare a compound of chemical formula 5. The carbodiimide compound is selected from 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride, 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide, 1,3-diisopropylcarbodiimide or 1,3-dicyclohexylcarbodiimide.

    Abstract translation: 目的:提供2-氰基-3-羟基-N - [(4-三氟甲基)苯基]丁-2-烯酰胺的制备方法,以便容易地除去最终产品的制造过程中产生的副产物。 构成:由化学式5的化合物制备化学式1的2-氰基-3-羟基-N - [(4-三氟甲基)苯基]丁-2-烯酰胺的方法包括以下步骤:活化化学式 式2与使用碳二亚胺化合物的酯化化合物反应; 将所得物与化学式4的化合物反应,制备化学式5的化合物。碳二亚胺化合物选自1- [3-(二甲基氨基)丙基] -3-乙基碳二亚胺盐酸盐,1- [3-(二甲基氨基) 丙基] -3-乙基碳二亚胺,1,3-二异丙基碳二亚胺或1,3-二环己基碳二亚胺。

    도네페질 중간체의 제조방법
    10.
    发明公开
    도네페질 중간체의 제조방법 无效
    一种制备多奈哌齐中间体的方法

    公开(公告)号:KR1020080092515A

    公开(公告)日:2008-10-16

    申请号:KR1020070035881

    申请日:2007-04-12

    CPC classification number: C07D211/32

    Abstract: A process for preparing an intermediate of donepezil having dementia-treating effects is provided to improve preparation yield and convenience of mass production of the intermediate by replacing the base which is difficult to be used industrially. An intermediate of donepezil, 2-[(E)-1-(1-benzyl-4-piperidyl)methylidene]-5,6-dimethoxy-1-indanone represented by the formula(1) is prepared by reacting 1-indanone compound represented by the formula(2) with aldehyde compound represented by the formula(3) by using a base selected from sodium methoxide(MeONa), sodium ethoxide(EtONa), potassium t-butoxide, sodium hydride, sodium hydroxide, potassium hydroxide and sodium amide in a reaction solvent selected from methanol, ethanol, isopropanol, t-butanol, tetrahydrofuran, 1,4-dioxane, diisopropyl ether, dimethylform amide, dimethylsulfoxide and nitromethane.

    Abstract translation: 提供一种制备具有痴呆症治疗效果的多奈哌齐中间体的方法,以通过更换难以在工业上使用的碱来改善中间体的制备产率和方便大量生产。 由式(1)表示的多奈哌齐2 - [(E)-1-(1-苄基-4-哌啶基)亚甲基] -5,6-二甲氧基-1-二氢茚酮的中间体是通过1- 由式(2)表示的醛与式(3)表示的醛化合物通过使用选自甲醇钠(MeONa),乙醇钠(EtONa),叔丁醇钾,氢化钠,氢氧化钠,氢氧化钾和钠 酰胺在选自甲醇,乙醇,异丙醇,叔丁醇,四氢呋喃,1,4-二恶烷,二异丙基醚,二甲基甲酰胺,二甲基亚砜和硝基甲烷的反应溶剂中。

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