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1. 发明授权

KR100472572B1 라세믹화합물의 비대칭 개환반응에 의한 키랄화합물의제조방법 失效
标题翻译：通过外消旋体不对称开环制备手性化合物
公开(公告)号：KR100472572B1
公开(公告)日：2005-03-07
申请号：KR1020010061831
申请日：2001-10-08
申请人： 주식회사 한솔케미칼
发明人： 이동훈 , 정다희 , 심우호 , 장석구 , 최두성 , 변일석
IPC分类号： C07D301/32
摘要： 본 발명은 키랄 살렌금속촉매하에서 라세믹 에폭시화합물의 비대칭 개환반응을 수행하여 입체선택성이 우수한 키랄 에폭사이드 또는 키랄 알코올과 같은 키랄화합물을 제조하는 방법에 있어, 키랄 살렌금속촉매의 활성화 및 안정화를 목적으로 때로는 반응용매겸 다음 화학식 1로 표시되는 화합물을 추가로 함유시키는데 그 특징이 있고, 이로써 고 광학순도의 키랄화합물을 얻으면서도 사용된 키랄살렌금속촉매를 고온에서도 안정한 상태로 보존하며 촉매를 분리하여 재사용시 촉매의 활성을 유지시키는 효과를 갖는다. 따라서, 키랄 살렌금속촉매와 화학식 1의 화합물이 함께 포함된 본 발명의 반응계는 기존의 키랄 살렌금속촉매 반응계와는 달리 첫 반응은 물론 재사용시에도 촉매를 활성화시키는 첨가물이 별도로 첨가될 필요없는 경제적이고 실용적인 시스템이다.
화학식 1

상기 화학식 1에서 : R, Y, n 및 A는 각각 발명의 상세한 설명에서 정의한 바와 같다.

2. 发明公开

KR1020040065830A 아르부틴 제조용 중간체의 제조방법 失效
标题翻译：制定ARBUTIN中间人的过程
公开(公告)号：KR1020040065830A
公开(公告)日：2004-07-23
申请号：KR1020030003017
申请日：2003-01-16
申请人： 주식회사 한솔케미칼
发明人： 이동훈 , 유용상 , 이광덕
IPC分类号： C07H15/203
摘要： PURPOSE: A process for preparing intermediates of arbutin is provided, thereby preparing no octaacetyl diglucosyl hydroquinone, reducing the preparation costs by beta-O-glycosylation of both mono-protected hydroquinone and di-protected hydroquinone, and improving the preparation yield of the arbutin intermediates. CONSTITUTION: The process for preparing intermediates of arbutin comprises reacting beta-D-glucose pentaacetate of formula (1) with mono- or di-trimethylsillyl hydroquinone of formula (2) in the presence of Lewis acid catalyst at 20 to 100 deg.C for 2 to 72 hours in a solvent to prepare beta-D-tetraacetylarbutin derivative of formula (3), wherein Ac is acetyl; R is trimethylsillyl; R1 and R2 are independently hydrogen or trimethylsillyl, provided that at least one of R1 and R2 is trimethylsillyl; the solvent is selected from toluene, xylene, benzene, dichloromethane, dichloroethane, chloroform, acetone, acetonitrile, hexane, cyclohexane or a mixture thereof; the Lewis acid is selected from tin tetrachloride, boron trifluoride, boron trichloride, zinc chloride, iron trichloride and trimethylsillyltrifluoromethanesulfonate.
摘要翻译：目的：提供一种制备熊果苷中间体的方法，由此不制备八乙酰基二葡糖基对苯二酚，通过单保护氢醌和二保护氢醌的β-O-糖基化降低制备成本，提高熊果苷中间体的制备产率。构成：制备熊果苷中间体的方法包括使式（1）的β-D-葡萄糖五乙酸酯与路易斯酸催化剂在20至100℃的存在下在式（2）的一或二 - 三甲基硅烷基氢醌反应，用于在溶剂中2至72小时以制备式（3）的β-D-四乙酰熊果苷衍生物，其中Ac为乙酰基; R是三甲基甲硅烷基; R1和R2独立地是氢或三甲基甲硅烷基，条件是R 1和R 2中的至少一个是三甲基甲硅烷基; 溶剂选自甲苯，二甲苯，苯，二氯甲烷，二氯乙烷，氯仿，丙酮，乙腈，己烷，环己烷或其混合物; 路易斯酸选自四氯化锡，三氟化硼，三氯化硼，氯化锌，三氯化铁和三甲基甲硅烷基三氟甲磺酸盐。

3. 发明公开

KR1020030066186A (Ｅ)-터비나핀 또는 이의 염산염의 제조방법 无效
标题翻译：生产（E） - 替硝基或其盐酸盐的方法
公开(公告)号：KR1020030066186A
公开(公告)日：2003-08-09
申请号：KR1020020006517
申请日：2002-02-05
申请人： 주식회사 한솔케미칼
发明人： 유용상 , 이동훈
IPC分类号： C07C209/68
摘要： PURPOSE: Provided is a method for economically and simply producing (E)-terbinafine represented by formula 1, or hydrochloride thereof with high yield and high purity, without removing a solvent. CONSTITUTION: The method comprises the steps of (i) reacting N-methyl-1-naphthalene amine or its hydrochloride and (E)-1,3-dichloropropene in aqueous organic solvent or its aqueous solution in the presence of weak base at 0-100 deg.C for 1-15 hours, to form (E)-N-(3-chloro-2-propenyl)-N-methyl-naphthalene methaneamine represented by formula 3; and sequentially adding 0.5-5 mol% of Cu and amine, and 3,3-dimethyl-1-butyne to the reaction product with using 0.5-5 mol% of palladium(Pd(II)) catalyst, to form (E)-terbinafine represented by formula 1 or its hydrochloride.
摘要翻译：目的：提供一种经济地和简单地生产以式（1）表示的（E） - 特比萘芬或其盐酸盐的方法，其高产率和高纯度，而不除去溶剂。方法：该方法包括以下步骤：（i）在弱碱存在下，在0-乙烯基吡啶存在下，使N-甲基-1-萘胺或其盐酸盐与（E）-1,3-二氯丙烯在有机溶剂水溶液或其水溶液中反应， 100℃下反应1-15小时，形成式（E）-N-（3-氯-2-丙烯基）-N-甲基 - 萘甲胺，由式3表示; 并使用0.5-5mol％的钯（Pd（II））催化剂依次向反应产物中加入0.5-5mol％的Cu和胺和3,3-二甲基-1-丁炔，形成（E） - 特比萘芬由式1或其盐酸盐代表。

4. 发明授权

KR100460453B1 아르부틴 제조용 중간체의 제조방법 失效
标题翻译： 아르부틴제조용중금체의제조방법
公开(公告)号：KR100460453B1
公开(公告)日：2004-12-08
申请号：KR1020030003017
申请日：2003-01-16
申请人： 주식회사 한솔케미칼
发明人： 이동훈 , 유용상 , 이광덕
IPC分类号： C07H15/203
摘要： PURPOSE: A process for preparing intermediates of arbutin is provided, thereby preparing no octaacetyl diglucosyl hydroquinone, reducing the preparation costs by beta-O-glycosylation of both mono-protected hydroquinone and di-protected hydroquinone, and improving the preparation yield of the arbutin intermediates. CONSTITUTION: The process for preparing intermediates of arbutin comprises reacting beta-D-glucose pentaacetate of formula (1) with mono- or di-trimethylsillyl hydroquinone of formula (2) in the presence of Lewis acid catalyst at 20 to 100 deg.C for 2 to 72 hours in a solvent to prepare beta-D-tetraacetylarbutin derivative of formula (3), wherein Ac is acetyl; R is trimethylsillyl; R1 and R2 are independently hydrogen or trimethylsillyl, provided that at least one of R1 and R2 is trimethylsillyl; the solvent is selected from toluene, xylene, benzene, dichloromethane, dichloroethane, chloroform, acetone, acetonitrile, hexane, cyclohexane or a mixture thereof; the Lewis acid is selected from tin tetrachloride, boron trifluoride, boron trichloride, zinc chloride, iron trichloride and trimethylsillyltrifluoromethanesulfonate.
摘要翻译：目的：提供一种制备熊果苷中间体的方法，由此制备无八乙酰基二葡萄糖基氢醌，通过单保护的氢醌和二保护的氢醌的β-O-糖基化来降低制备成本，并且提高熊果苷中间体的制备产率。构成：制备熊果苷中间体的方法包括使式（1）的β-D-葡萄糖五乙酸酯与式（2）的单 - 或二 - 三甲基甲硅烷基氢醌在路易斯酸催化剂存在下在20-100℃ 在溶剂中2-72小时以制备式（3）的β-D-四乙酰基丁胺衍生物，其中Ac为乙酰基; R是三甲基甲硅烷基; R1和R2独立地为氢或三甲基甲硅烷基，条件是R1和R2中的至少一个为三甲基甲硅烷基; 溶剂选自甲苯，二甲苯，苯，二氯甲烷，二氯乙烷，氯仿，丙酮，乙腈，己烷，环己烷或其混合物; 路易斯酸选自四氯化锡，三氟化硼，三氯化硼，氯化锌，三氯化铁和三甲基硅基三氟甲磺酸盐。

5. 发明公开

KR1020020092502A 에피클로로히드린의 비대칭 고리열림 반응에 의한 키랄화합물 제조방법 无效
标题翻译：通过不对称开环化学反应制备化合物的方法
公开(公告)号：KR1020020092502A
公开(公告)日：2002-12-12
申请号：KR1020010031150
申请日：2001-06-04
申请人： 주식회사 한솔케미칼 , 주식회사 씨트리
发明人： 이동훈 , 장석구 , 함철 , 정다희 , 심우호 , 변일석 , 최두성
IPC分类号： C07D301/32
摘要： PURPOSE: Provided is a process for manufacturing chiral compounds by asymmetric ring opening reaction of racemic Epichlorohydrin with nucleophile in the presence of a chiral catalyst, in high yield and optical purity. CONSTITUTION: The process for manufacturing chiral compound comprises the steps of: asymmetric ring opening reaction of racemic Epichlorohydrin with a nucleophile in the presence of a chiral catalyst of the formula(1) in a solvent containing a salt of the formula(2) or (3) or within a solvent system containing a mixture of the compounds of the formula(2) and formula(3); and separating a reaction product from the catalyst, wherein DKR(dynamic kinetic resolution) reaction is characteristically involved.
摘要翻译：目的：提供在手性催化剂存在下，以高产率和光学纯度，通过外消旋表氯醇与亲核试剂的不对称开环反应制备手性化合物的方法。构成：制备手性化合物的方法包括以下步骤：在含有式（2）的盐或（2）的盐的溶剂中，在式（1）的手性催化剂的存在下，外消旋的表氯醇与亲核试剂的不对称开环反应， 3）或在含有式（2）和式（3）的化合物的混合物的溶剂体系内; 并从催化剂中分离反应产物，其特征在于涉及DKR（动态动力学拆分）反应。

6. 发明公开

KR1020030034287A 라세믹화합물의 비대칭 개환반응에 의한 키랄화합물의제조방법 失效
标题翻译：通过选择性环开放化合物反应的化合物的方法
公开(公告)号：KR1020030034287A
公开(公告)日：2003-05-09
申请号：KR1020010061831
申请日：2001-10-08
申请人： 주식회사 한솔케미칼
发明人： 이동훈 , 정다희 , 심우호 , 장석구 , 최두성 , 변일석
IPC分类号： C07D301/32
摘要： PURPOSE: A process for preparing chiral compounds by enantioselective ring opening reaction of racemic compounds is provided, the high optical purity of chiral compounds can be prepared, and enzyme used can be reused. CONSTITUTION: The process for preparing chiral compounds such as chiral epoxide or chiral alcohol by enantioselective ring opening reaction of racemic epoxy compounds in a chiral salen metal catalyst reaction system comprises further containing a compound represented by formula(1):((R-SO2)n-Y)(A) in the chiral salen metal catalyst reaction system, wherein R is halogen atom, alkyl, aryl or haloalkyl; Y is oxygen or nitrogen wherein n is 1 when Y is oxygen or n is 2 when Y is nitrogen; and A is a counter ion including hydrogen, halogen, alkali metal atom, or grade 4 ammonium.
摘要翻译：目的：提供通过外消旋化合物的对映选择性开环反应制备手性化合物的方法，可以制备手性化合物的高光学纯度，并且可以重复使用酶。构成：手性盐金属催化剂反应体系中外消旋环氧化合物的对映选择性开环反应制备手性化合物如手性环氧化物或手性醇的方法还包含由式（1）表示的化合物：（（R-SO 2） nY）（A）在手性salen金属催化剂反应体系中，其中R是卤素原子，烷基，芳基或卤代烷基; Y是氧或氮，当Y是氧时n是1，当Y是氮时，n是2; A是包括氢，卤素，碱金属原子或4级铵的抗衡离子。

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