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1. 发明授权

KR100543542B1 4-안드로스텐-3,17-디온으로부터 구굴스테론의 제조방법및 이를 제조하기 위한 중간체 失效
标题翻译：用于制备4,1720-前四环素-3,16-二酮的方法，由4-安慰剂-3,17-二酮和用于制备其的中间体化合物
公开(公告)号：KR100543542B1
公开(公告)日：2006-01-20
申请号：KR1020030025936
申请日：2003-04-24
申请人： 강헌중
发明人： 강헌중 , 함정엽 , 진정욱
IPC分类号： C07J13/00
摘要： 본 발명은 4-안드로스텐-3,17-디온으로부터 인간의 저밀도 지방단백질(LDL; low density lipoprotein) 및 콜레스테롤 수치를 효과적으로 낮추고, 고밀도 지방단백질(HDL; high density lipoprotein)을 높이는 일반식(VI)으로 표시되는 4,17(20)-
E -프로스타디엔-3,16-디온(
E -Guggulesterone;
E -구굴스테론) 및 일반식(VII)로 표시되는 4,17(20)-
Z -프로스타디엔-3,16-디온(
Z -Guggulesterone;
Z -구굴스테론)의 제조방법을 제공한다.
또한, 본 발명은 화합물 (VI)과 (VII)을 제조하기 위한 중간체인 상기 일반식(III), (V), (VIII) 및 (IX)를 합성하는 방법을 제공한다.

2. 发明公开

KR1020050078660A 4,17(20)-이-프로스타디엔-3,16-디온의 제조방법 및 이를제조하기 위한 중간체 失效
标题翻译：制备4,17（20）-E-前三苯基-3,16-二酮的方法和用于制备其的中间体化合物
公开(公告)号：KR1020050078660A
公开(公告)日：2005-08-05
申请号：KR1020050063669
申请日：2005-07-14
申请人： 강헌중
发明人： 강헌중
IPC分类号： C07J13/00
CPC分类号： C07J13/00 , C07J7/0005
摘要： 본 발명은 인간의 저밀도 지방단백질(LDL; low density lipoprotein) 및 콜레스테롤 수치를 효과적으로 낮추고, 고밀도 지방단백질(HDL; high density lipoprotein)을 높이는 것으로 알려진 일반식(IV)로 표시되는 4,17(20)-
E -프로스타디엔-3,16-디온(
E -Guggulsterone;
E -구굴스테론)의 제조방법을 제공한다. 본 발명의 방법중 중간체인 일반식(VI)은 신규물질이다.

3. 发明授权

KR100639655B1 16α,17α-에폭시프레그네놀론으로부터4,17(20)-프로스타디엔-3,16-디온의 제조방법 및 이를제조하기 위한 중간체 有权
标题翻译：从16α，17β-羟基丙酮制备4,1720-前二苯并-3,16-二酮的方法和用于制备其的中间体化合物
公开(公告)号：KR100639655B1
公开(公告)日：2006-10-30
申请号：KR1020030025904
申请日：2003-04-24
申请人： 강헌중
发明人： 강헌중 , 함정엽 , 진정욱
IPC分类号： C07J13/00
摘要： 본 발명은 16α,17α-에폭시프레그네놀론(I)로부터 인간의 저밀도 지방단백질(LDL; low density lipoprotein) 및 콜레스테롤 수치를 효과적으로 낮추고, 고밀도 지방단백질(HDL; high density lipoprotein)을 높이는 것으로 알려진 일반식 (Ⅲ)으로 표시되는 4,17(20)-
E -프로스타디엔-3,16-디온 만을 선택적으로 제조하는 방법을 제공한다.

4. 发明公开

KR1020040092078A 5-안드로스텐-3β-올-17-온으로부터4,17(20)-프로스타디엔-3,16-디온의 제조방법 및 이를제조하기 위한 중간체 失效
标题翻译：用于制备具有高效率的短时间反应时间的5-ANDROSTENE-3BETA-OL-17-ONE和中间体化合物的4,17（20） - 丙烯三烯-3,16-二醇的方法
公开(公告)号：KR1020040092078A
公开(公告)日：2004-11-03
申请号：KR1020030025919
申请日：2003-04-24
申请人： 강헌중
发明人： 강헌중 , 함정엽 , 진정욱
IPC分类号： C07J13/00
CPC分类号： C07J13/007 , A61K31/56 , B01J31/0225
摘要： PURPOSE: A process for preparing 4,17(20)-prostadien-3,16-dione from 5-androstene-3beta-ol-17-one and intermediate compounds for preparing the same are provided to lower values for low density lipoprotein and cholesterol and to increase a value for high density lipoprotein. CONSTITUTION: The process for preparing 4,17(20)-prostadien-3,16-dione(E-guggulsterone) represented by formula IV comprises the steps of: reacting 5-androstene-3beta-ol-17-one represented by formula I with an ethyltriphenyl phosphonium halide under a presence of a strong base to obtain a compound represented by formula II; introducing a hydroxy group to C-16 position of the obtained compound to obtain a compound represented by formula III; and oxidizing it.
摘要翻译：目的：从5-雄甾烯-3β-ol-17-一制备4,17（20） - 前列腺素-3,16-二酮及其制备方法，用于低密度脂蛋白和胆固醇的较低值并增加高密度脂蛋白的价值。构成：由式IV表示的制备4,17（20） - 前草酮-3,16-二酮（E-guccersterone）的方法包括以下步骤：将由式I表示的5-雄甾烯-3β-醇-17- 与乙基三苯基鏻卤化物在强碱存在下反应得到式II表示的化合物; 将所得化合物的羟基引入C-16位，得到式III表示的化合物; 并氧化它。

5. 发明公开

KR1020040092066A 16α,17α-에폭시프레그네놀론으로부터4,17(20)-프로스타디엔-3,16-디온의 제조방법 및 이를제조하기 위한 중간체 有权
标题翻译：制备4,17（20） - 十六烷基-3,16-二酮的方法，由16种ALPHA，17种ALPHA-EPOXYPREGNENOLONE和中间体化合物制备相当于短效反应时间的高效率
公开(公告)号：KR1020040092066A
公开(公告)日：2004-11-03
申请号：KR1020030025904
申请日：2003-04-24
申请人： 강헌중
发明人： 강헌중 , 함정엽 , 진정욱
IPC分类号： C07J13/00
CPC分类号： C07J13/007 , A61K31/56 , C07B33/00
摘要： PURPOSE: A process for preparing 4,17(20)-prostadien-3,16-dione from 16 alpha, 17 alpha-epoxypregnenolone are provided to effectively lower the values for low density lipoprotein and cholesterol and to increase the value for high density lipoprotein. CONSTITUTION: The process for preparing 4,17(20)-prostadien-3,16-dione(E-guggulsterone) represented by formula III from 16 alpha, 17 alpha-epoxypregnenolone comprises the steps of: reacting 16 alpha, 17 alpha-epoxypregnenolone represented by formula I with a hydrazine to obtain a compound represented by formula II, wherein 1 to 40 equivalent of the hydrazine is used to the 16 alpha, 17 alpha-epoxypregnenolone; and then oxidizing it using aluminum alkoxides.
摘要翻译：目的：提供从16α，17α-环氧孕烯醇酮制备4,17（20） - 前列腺素-3,16-二酮的方法，以有效降低低密度脂蛋白和胆固醇的值，并增加高密度脂蛋白的值。构成：由16α，17α-环氧孕烯醇酮制备由式III代表的4,17（20） - 前病毒-3,16-二酮（E-guccersterone）的方法包括以下步骤：使16α，17α-环氧孕烯醇酮由式I与肼反应，得到式II表示的化合物，其中将1〜40当量的肼用于16α，17α-环氧孕烯醇; 然后用烷氧基铝氧化。

6. 发明公开

KR1020030086373A 티아졸 유도체의 제조방법 및 이를 제조하기 위한 중간체 失效
标题翻译：制备噻唑衍生物的方法及其制备中间体
公开(公告)号：KR1020030086373A
公开(公告)日：2003-11-10
申请号：KR1020020024595
申请日：2002-05-04
申请人： 강헌중 , 함정엽
发明人： 강헌중 , 함정엽
IPC分类号： C07D277/36
CPC分类号： C07C323/20 , C07D277/26 , Y02P20/55
摘要： PURPOSE: A process for preparing thiazole derivatives and intermediates for the preparation thereof are provided, thereby easily preparing the thiazole derivatives in higher yield. CONSTITUTION: A process for preparing 2 - {2 - methyl - 4 - £({4 - methyl - 2 - £4 - (trifluoromethyl) phenyl| - 1,3 - thiazole - 5 - yl}methyl)sulfanyl|phenoxy} acetate of the formula (X) comprises the steps of: reacting a compound of the formula (III) with a compound of the formula (VI) to prepare a compound of the formula (VII); removing a protecting group from the compound of the formula (VII) to prepare a compound of the formula (VIII); reacting the compound of the formula (VIII) with halogenacetic acid alkylester to prepare a compound of the formula (IX); and hydrolysis of the compound of the formula (IX), wherein R1 is C1-C4 alkyl, alkyl or aralkylsilyl phenol protecting group; R2 is hydrogen and methyl; R3 is C1-C4 alkyl containing carboxylic acid protecting group; X1 is halogen atom and hydrogen atom; X2 is halogen atom and a releasing group having improved reactivity in electron affinity reaction; and M is lithium and magnesium ions. Intermediates for the preparation thereof include the thiazole derivative of formula (III) or formula (VII).
摘要翻译：目的：提供制备噻唑衍生物的方法及其制备中间体，从而以更高的收率容易地制备噻唑衍生物。构成：制备2- {2-甲基-4 - （（4-甲基-2-（4-（三氟甲基）苯基] -1,3-噻唑-5-基}甲基）硫烷基|苯氧基}乙酸酯的方法式（X）的化合物包括以下步骤：使式（III）的化合物与式（VI）的化合物反应以制备式（VII）的化合物; 从式（Ⅶ）化合物中除去保护基以制备式（Ⅷ）化合物; 使式（Ⅷ）化合物与卤代乙酸烷基酯反应制备式（Ⅸ）化合物; 和其中R 1是C 1 -C 4烷基，烷基或芳烷基甲硅烷基苯酚保护基的式（Ⅸ）化合物的水解; R2是氢和甲基; R3是含羧酸保护基的C1-C4烷基; X1是卤原子和氢原子; X2是卤素原子，在电子亲和反应中具有改善的反应性的释放基团; M是锂离子和镁离子。用于制备其的中间体包括式（III）或式（VII）的噻唑衍生物。

7. 发明公开

KR1020060029176A 페록시솜 증식자 활성화 수용체 델타 리간드의 제조방법 및이를 제조하기 위한 중간체 失效
标题翻译：制备PPARA配体和中间体化合物的制备方法
公开(公告)号：KR1020060029176A
公开(公告)日：2006-04-04
申请号：KR1020060024792
申请日：2006-03-17
申请人： 강헌중
发明人： 강헌중 , 함정엽
IPC分类号： C07F3/02
CPC分类号： C07F3/02 , C07D277/26 , C07F19/00
摘要： 본 발명은 인간의 페록시솜 증식자 활성화 수용체 δ(peroxisome proliferator activated receptor δ: hPPARδ)에 활성을 갖는 일반식(I)로 표시되는 티아졸 유도체를 고수율로 제조하는 신규의 방법 및 이 방법을 수행하기 위한 중간체인 일반식(II), (IV), (X), (XI) 및 (XII)과 이들의 합성방법을 제공한다.

8. 发明公开

KR1020040105422A 해양성 와편모조류 린구로디늄 폴리에드룸으로부터 디에이치에이 및 이피에이의 제조방법 失效
标题翻译：通过具有高纯度和高YIELD的简单加工步骤从海洋DINOFLAGELLATE，LINGULODINIUM POLYEDRUM制备DHA和EPA的方法
公开(公告)号：KR1020040105422A
公开(公告)日：2004-12-16
申请号：KR1020030036793
申请日：2003-06-09
申请人： 강헌중 , 정해진
发明人： 강헌중 , 정해진 , 김재성 , 원동환 , 남상집
IPC分类号： C11B1/10
CPC分类号： C11B1/10 , C11B1/04
摘要： PURPOSE: Provided is a method for preparing DHA(docosahexaenoic acid) and EPA(eicosapentaenoic acid) useful for food additives, which uses Lingulodinium polyedrum as a starting material to produce DHA and EPA with high purity and high yield. CONSTITUTION: The method for preparing DHA and EPA uses a dry product containing DHA and EPA obtained by freeze drying Lingulodinium polyedrum, which is dinoflagellate. The method comprises the steps of: extracting the dry product with a mixed solvent; evaporating the organic solvent layer under reduced pressure and purifying the resultant product by chromatography, or evaporating the solvent under reduced pressure and extracting the resultant residue with lower alcohol/C6-8 alkane solvent, so that fractions of lower alcohol layer can be obtained; evaporating the fractions to remove the solvent; extracting the resultant residue with ethyl acetate/water to obtain the ethyl acetate layer; mixing the ethyl acetate layer with the C6-8 alkane layer; evaporating the resultant mixture under reduced pressure and purifying the residue by chromatography.
摘要翻译：目的：提供一种可用于食品添加剂的DHA（二十二碳六烯酸）和EPA（二十碳五烯酸）的制备方法，该方法以高纯度和高产率生产DHA和EPA为起始原料。构成：用于制备DHA和EPA的方法使用含有DHA和EPA的干燥产品，其通过冷冻干燥葡萄柚多糖得到。该方法包括以下步骤：用混合溶剂萃取干燥产物; 在减压下蒸发有机溶剂层，通过色谱法纯化所得产物，或在减压下蒸发溶剂，并用低级醇/ C6-8烷烃溶剂萃取所得残余物，从而可得到低级醇层级分; 蒸发馏分以除去溶剂; 用乙酸乙酯/水萃取所得残留物，得到乙酸乙酯层; 将乙酸乙酯层与C6-8烷烃层混合; 在减压下蒸发所得混合物并通过色谱法纯化残余物。

9. 发明公开

KR1020040092518A 프로제스테론으로부터 구굴스테론의 제조방법 및 이를제조하기 위한 중간체 失效
标题翻译：用于制备前列腺素的方法，用于制备低密度脂蛋白和胆固醇的下限值的PROGESTERONE和中间体化合物
公开(公告)号：KR1020040092518A
公开(公告)日：2004-11-04
申请号：KR1020030025989
申请日：2003-04-24
申请人： 강헌중
发明人： 강헌중 , 함정엽 , 진정욱
IPC分类号： C07J13/00
CPC分类号： C07J13/007 , A61K31/56 , C07B31/00 , C07B33/00
摘要： PURPOSE: A process for preparing 4,17(20)-prostadien-3,16-dione from progesterone and intermediate compounds for preparing the same are provided to lower values for low density lipoprotein and cholesterol and to increase a value for high density lipoprotein. CONSTITUTION: The process for preparing 4,17(20)-prostadien-3,16-dione represented by formula VII from progesterone comprises the steps of: reducing the progesterone represented by formula I; oxidizing with a manganese dioxide; reacting with a methane sulfonyl chloride or p-toluene sulfonyl chloride; olefinating by treating the obtained compound with a strong base; selective oxidizing with a selenium compound and a peroxide; and oxidizing it.
摘要翻译：目的：从孕酮和中间体化合物制备4,17（20） - 前列腺素-3,16-二酮的制备方法可用于降低低密度脂蛋白和胆固醇的含量，并增加高密度脂蛋白的价值。构成：由孕酮制备由式VII代表的4,17（20） - 前列腺素-3,16-二酮的方法包括以下步骤：减少由式I表示的孕酮; 用二氧化锰氧化; 与甲磺酰氯或对甲苯磺酰氯反应; 用强碱处理得到的化合物进行烯化; 用硒化合物和过氧化物选择性氧化; 并氧化它。

10. 发明公开

KR1020040092500A 테스토스테론으로부터 구굴스테론의 제조방법 및 이를제조하기 위한 중간체 失效
标题翻译：用于制备具有增加高密度脂蛋白的价值的蛋白质和中间体化合物的前体化合物的方法
公开(公告)号：KR1020040092500A
公开(公告)日：2004-11-04
申请号：KR1020030025962
申请日：2003-04-24
申请人： 강헌중
发明人： 강헌중 , 함정엽 , 진정욱
IPC分类号： C07J13/00
CPC分类号： C07J13/007 , A61K31/56 , B01J31/0225
摘要： PURPOSE: A process for preparing 4,17(20)-prostadien-3,16-dione from testosterone and intermediate compounds for preparing the same are provided to lower values for low density lipoprotein and cholesterol and to increase a value for high density lipoprotein. CONSTITUTION: The process for preparing 4,17(20)-E-prostadien-3,16-dione represented by formula VII from testosterone comprises the steps of: reacting testosterone represented by formula I with an alkane diol under a presence of an acid catalyst; reacting with a chrome oxide; reacting with an ethyl triphosphonium halide and a strong base; de-protecting; oxidizing with a selenium compound and a peroxide; and oxidizing it with a manganese oxide.
摘要翻译：目的：提供从睾丸酮制备4,17（20） - 前列腺素-3,16-二酮的方法及其制备中间体化合物的方法，以降低低密度脂蛋白和胆固醇的含量，并增加高密度脂蛋白的价值。构成：从睾丸酮制备由式Ⅶ表示的4,17（20）-E-前列腺素-3,16-二酮的方法包括以下步骤：在酸催化剂存在下使式I表示的睾酮与烷二醇反应 ; 与氧化铬反应; 与乙基三卤化鏻和强碱反应; 去保护; 用硒化合物和过氧化物氧化; 并用氧化锰氧化。

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