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    • 21. 发明公开
    • 항진균제용 터비나핀 및 그 염산염의 제조방법
    • 生产用于抗真菌药物的丝氨酸蛋白酶及其盐酸盐的方法
    • KR1020020016276A
    • 2002-03-04
    • KR1020000049521
    • 2000-08-25
    • 주식회사 씨트리
    • 백용구김경수이동우유정복박성준김완주
    • C07C209/10
    • PURPOSE: Provided is a process for producing terbinafine and hydrochloride thereof used as an antifungal agent, which can be used for oral administration and hardly has toxicity. CONSTITUTION: The process comprises the steps of: preparing a halide intermediate by reacting 6,6-dimethyl-2-(E)-heptene-4-ynil alcohol(formula III) and a halogenating agent such as SOCl2, SOBr2, HCl, HBr, PCl3, PCl5, and etc.; preparing (E)-N-(6,6-dimethyl-2-heptyne-4-ynil)-N-methyl-1-naphthaleneamine(terbinafine)(formula I) by reacting the halide intermediate(formula IV) with N-methyl-1-naphthalene methanamine in the presence of potassium carbonate; preparing the hydrochloride(formula II) of the terbinafine by acidifying the terbinafine in a methanolic HCl solution and then performing recrystallization.
    • 目的:提供用作抗真菌剂的特比萘芬和盐酸盐的制备方法,其可用于口服给药,几乎不具有毒性。 方法:该方法包括以下步骤:通过使6,6-二甲基-2-(E) - 庚烯-4-炔醇(式III)和卤化剂如SOCl 2,SOBr 2,HCl,HBr反应制备卤化物中间体 ,PCl3,PCl5等; 通过使卤化物中间体(式IV)与N-甲基(式II)反应制备(E)-N-(6,6-二甲基-2-庚炔-4-基)-N-甲基-1-萘胺(特比萘芬)(式I) -1-萘甲胺在碳酸钾存在下反应; 通过在甲醇HCl溶液中酸化特比萘芬,然后进行重结晶,制备特比萘芬的盐酸盐(式II)。
    • 22. 发明公开
    • 산도에 민감한 중합체를 이용한 달걀 면역 항체의캡슐화방법
    • 使用聚合物对酸性敏感的蛋黄免疫球蛋白包埋方法
    • KR1020010081232A
    • 2001-08-29
    • KR1020000006415
    • 2000-02-11
    • 주식회사 씨트리
    • 김완주김경수이유정요시노리미네
    • A61K9/48
    • Y02A50/473Y02A50/481Y02A50/483A61K9/5026A61K9/4833A61K39/395A61K2039/505
    • PURPOSE: A method for encapsulating egg yolk antibodies IgY by using a methacrylate monomer or polymer solution sensitive to acidity is provided, which increases stability to heat, low pH such as gastric acid and proteinase present in an alimentary system. CONSTITUTION: Encapsulation method of egg yolk immunoglobulins (IgY) comprises adding 0.1 to 10% methacrylate monomer or polymer solution to egg yolk containing specific antibodies and freeze-drying. The specific antibodies are anti-H. pylori IgY, anti-Rotavirus IgY, anti-enterotoxigenic E. coli IgY, anti-Y. reckeri IgY, anti-Edward tarda IgY, anti-Edward siella Igy, anti-Vibrio Igy, anti-Salmonella gallinarum IgY, anti-Salmonella enteritidis IgY, anti-Streptococcus iniae IgY and anti-Fowl Typhoid IgY.
    • 目的:提供一种通过使用对酸度敏感的甲基丙烯酸酯单体或聚合物溶液来包封蛋黄抗体IgY的方法,其增加了耐热性,低pH(例如存在于消化系统中的胃酸和蛋白酶)的稳定性。 构成:蛋黄免疫球蛋白(IgY)的包封方法包括向含有特异性抗体的蛋黄中加入0.1〜10%的甲基丙烯酸酯单体或聚合物溶液并进行冷冻干燥。 特异性抗体为抗H。 幽门螺杆菌IgY,抗轮状病毒IgY,抗肠毒素性大肠杆菌IgY,抗Y。 reckeri IgY,抗Edward tarda IgY,抗Edward siella Igy,抗弧菌Igy,抗沙门氏菌IgY,抗肠炎沙门氏菌IgY,抗链球菌IgY和抗家禽伤寒IgY。
    • 23. 发明公开
    • 항진균제용 터비나핀 및 그 염산염의 제조방법
    • 作为抗生素剂及其盐酸盐的生产酪氨酸蛋白酶
    • KR1020000065691A
    • 2000-11-15
    • KR1019990012298
    • 1999-04-08
    • 주식회사 씨트리한솔케미언스 주식회사고려제약주식회사
    • 이태석안현숙유창현김경수육진수오성수주소경김완주
    • C07C209/68
    • PURPOSE: A process for preparing the titled compound by using N-methyl-1-naphthalenemethaneamine or its hydrochloric acid salt and 1,3-dichloropropene as a starting material and reacting in the presence of a palladium catalyst system and an alkali is provided which produces a terbinafine compound in high yield and inhibits side reactions. CONSTITUTION: N-methyl-1-naphthalenemethaneamine or its hydrochloric acid salt and 1,3-dichloropropene are reacted with 0.5 to 5% by mole of a palladium catalyst selected from (PPh3)2PdCl2, (PhCN)2PdCl2 or (PPh3)4Pd in a nonpolar solvent in the presence of an alkali at 0 to 50°C for 1 to 2 hr to give N-methyl-N-(3-chloro-1-propene-2-yl)-naphthalenemethaneamine of formula (II), which is added with cul and amine, 3,3-dimethyl-1-butine successively to give (E)-terbinafine of formula (I).
    • 目的:提供使用N-甲基-1-萘甲烷或其盐酸盐和1,3-二氯丙烯作为原料并在钯催化剂体系和碱的存在下反应制备标题化合物的方法,其产生 特比萘芬化合物高产量并抑制副反应。 构成:将N-甲基-1-萘甲烷或其盐酸盐和1,3-二氯丙烯与0.5〜5摩尔%的选自(PPh 3)2 PdCl 2,(PhCN)2 PdCl 2或(PPh 3)4 Pd的钯催化剂反应, 非碱性溶剂,在碱存在下,在0〜50℃下反应1〜2小时,得到式(II)的N-甲基-N-(3-氯-1-丙烯-2-基) - 萘甲烷胺,其中 加入苦味胺和3,3-二甲基-1-丁胺,得到式(I)的(E) - 喋呤。
    • 27. 发明公开
    • 마이크로리엑터를 이용한 리싸이클 코발트 자성 이온성 액체의 제조
    • 使用微机的回收钴离子液体的合成
    • KR1020130102269A
    • 2013-09-17
    • KR1020120023375
    • 2012-03-07
    • 주식회사 씨트리
    • 유정복이주원육덕수이덕희장국진김현지주소경김완주
    • C01G51/00B01J3/00B01J19/24
    • PURPOSE: A synthesis method of cobalt magnetic ionic liquid is provided to manufacture the magnetic anionic liquid having various physical properties by synthesizing the cobalt magnetic ionic liquid continuously and safely using a microreactor. CONSTITUTION: A synthesis method of recycle cobalt magnetic ionic liquid comprises a step of reacting the cation and anion using a microreactor. The magnetic ionic liquid contains Co ion in the anion part. The cation is one compound selected from a group consisting of alkylimidazolium, alkylpyrrolidinium, alkylpyridinium, tetraalkylammonium, and tetraalkylphosphonium. The reaction temperature including the microreactor is 0-100°C. The application concentration of the cation and anion is 0.0002-1.0 mole. [Reference numerals] (AA) 1 week; (BB) 2 weeks; (CC) 3 weeks; (DD) 4 weeks; (EE) 6 weeks; (FF) 8 weeks; (GG) 10 weeks
    • 目的:提供钴磁性离子液体的合成方法,通过使用微反应器连续且安全地合成钴磁性离子液体来制造具有各种物理性质的磁性阴离子液体。 构成:回收钴磁性离子液体的合成方法包括使用微反应器使阳离子和阴离子反应的步骤。 磁离子液体在阴离子部分含有Co离子。 阳离子是选自烷基咪唑鎓,烷基吡咯烷鎓,烷基吡啶鎓,四烷基铵和四烷基鏻的一种化合物。 包括微反应器的反应温度为0-100℃。 阳离子和阴离子的应用浓度为0.0002-1.0摩尔。 (附图标记)(AA)1周; (BB)2周; (CC)3周; (DD)4周; (EE)6周; (FF)8周; (GG)10周
    • 29. 发明公开
    • 마이크로리엑터를 사용한 할라이드 함유량이 적은 포스포늄계-이온성 액체의 합성
    • 使用微波反应器合成具有低卤含量的基于磷的离子液体
    • KR1020120114545A
    • 2012-10-17
    • KR1020110032122
    • 2011-04-07
    • 주식회사 씨트리
    • 유정복주정재육덕수이주원김석인주소경김완주
    • C07F9/54C07C305/06C07C309/06B01J19/00
    • B01D53/1493B01D53/1475C07F9/5442
    • PURPOSE: A synthesis method of phosphonium based-ionic liquid which includes small amount of halide using a micro reactor is provided to efficiently relieve complex reaction condition of the manufacturing method. CONSTITUTION: A synthesis method of phosphonium based-ionic liquid includes a step of reacting cation - provided phosphonium compound with dimethyl sulfate, trifluoro methane sulfate, or negative ion-provided compound of iodine alkane by using a micro reactor. The cation - provided phosphonium compound is trimethyl phosphine, triethylene phosphin, tripropylphosphine, tributyl phosphine or triphenylphosphine. The manufacturing method includes a step of separately vacuum evaporating the ionic liquid which came out after being reacted. The application concentration of the cation - provided phosphonium compound is 0.0002-1.0 mole, and the application concentration of the negative ion - provided compound is 0.0002-1.0 mole.
    • 目的:提供使用微反应器包含少量卤化物的鏻基离子液体的合成方法,以有效缓解制备方法的复杂反应条件。 构成:鏻基离子液体的合成方法包括使用微反应器使阳离子提供的鏻化合物与硫酸二甲酯,三氟甲烷硫酸盐或负烷基碘烷烃化合物反应的步骤。 阳离子提供的鏻化合物是三甲基膦,三亚乙基膦,三丙基膦,三丁基膦或三苯基膦。 该制造方法包括分别真空蒸发反应后出来的离子液体的步骤。 阳离子提供的鏻化合物的应用浓度为0.0002-1.0摩尔,负离子提供化合物的应用浓度为0.0002-1.0摩尔。
    • 30. 发明授权
    • 디아세트아미도콜히친 및/또는 디아세트아미도디히드로티오콜히친을 함유하는 약제학적 조성물 및 이들 화합물의 제조방법
    • 含有脱乙酰焦醇和/或脱乙酰氨基羟基胆碱的药物组合物及其制备方法
    • KR100847565B1
    • 2008-07-21
    • KR1020070054843
    • 2007-06-05
    • 주식회사 씨트리
    • 윤은영이건봉장동조김순옥김완주
    • A61K31/122A61P37/06
    • A pharmaceutical composition containing deacetamidocolchicine, deacetamidodehydrothiocolchicine or a mixture thereof is provided to suppress immune responses and treat skin or organ transplant rejection without side effects. A method for preparing the compounds is also provided to eliminate separation of isomers and improve preparation yield. A pharmaceutical composition for suppressing immune responses and treating skin or organ transplant rejection contains deacetamidocolchicine, deacetamidodehydrothiocolchicine or a mixture thereof, wherein the deacetamidodehydrothiocolchicine is prepared by reacting 7-hydroxycolchicine with trifluoromethyl sulfonyl chloride in solvent, and the deacetamidocolchicine is prepared by reacting deacetamidodehydrothiocolchicine with NBSH(nitrobenzene sulfonyl hydrazide).
    • 提供含有脱乙酰胺秋水仙素,脱乙酰胺脱水硫代秋水仙碱或其混合物的药物组合物以抑制免疫应答并治疗皮肤或器官移植排斥而没有副作用。 还提供了制备该化合物的方法以消除异构体的分离并提高制备产率。 用于抑制免疫应答和治疗皮肤或器官移植排斥的药物组合物含有脱乙酰胺基智可碱,脱乙酰胺脱水硫代秋水仙碱或其混合物,其中脱乙酰胺脱水硫代秋水仙素通过7-羟基秋水仙素与三氟甲基磺酰氯在溶剂中反应制备,脱乙酰胺基智可碱通过使脱乙酰胺基二硫代水葫芦素与NBSH (硝基苯磺酰肼)。