公开(公告)号：KR1020040092078A

公开(公告)日：2004-11-03

申请号：KR1020030025919

申请日：2003-04-24

Applicant: 강헌중

Inventor： 강헌중 ,  함정엽 ,  진정욱

IPC: C07J13/00

CPC classification number: C07J13/007 ,  A61K31/56 ,  B01J31/0225

Abstract: 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.

Abstract translation: 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。

公开(公告)号：KR1020040092066A

公开(公告)日：2004-11-03

申请号：KR1020030025904

申请日：2003-04-24

Applicant: 강헌중

Inventor： 강헌중 ,  함정엽 ,  진정욱

IPC: C07J13/00

CPC classification number: C07J13/007 ,  A61K31/56 ,  C07B33/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：KR1020060029176A

公开(公告)日：2006-04-04

申请号：KR1020060024792

申请日：2006-03-17

Applicant: 강헌중

Inventor： 강헌중 ,  함정엽

IPC: C07F3/02

CPC classification number: C07F3/02 ,  C07D277/26 ,  C07F19/00

Abstract: 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.

公开(公告)号：KR1020040105422A

公开(公告)日：2004-12-16

申请号：KR1020030036793

申请日：2003-06-09

Applicant: 강헌중 ,  정해진

Inventor： 강헌중 ,  정해진 ,  김재성 ,  원동환 ,  남상집

IPC: C11B1/10

CPC classification number: C11B1/10 ,  C11B1/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：KR1020040092518A

公开(公告)日：2004-11-04

申请号：KR1020030025989

申请日：2003-04-24

Applicant: 강헌중

Inventor： 강헌중 ,  함정엽 ,  진정욱

IPC: C07J13/00

CPC classification number: C07J13/007 ,  A61K31/56 ,  C07B31/00 ,  C07B33/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：KR1020040092500A

公开(公告)日：2004-11-04

申请号：KR1020030025962

申请日：2003-04-24

Applicant: 강헌중

Inventor： 강헌중 ,  함정엽 ,  진정욱

IPC: C07J13/00

CPC classification number: C07J13/007 ,  A61K31/56 ,  B01J31/0225

Abstract: 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.

Abstract translation: 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。

公开(公告)号：KR100543553B1

公开(公告)日：2006-01-20

申请号：KR1020050063669

申请日：2005-07-14

Applicant: 강헌중

Inventor： 강헌중

IPC: C07J13/00

Abstract: 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.

公开(公告)号：KR100543544B1

公开(公告)日：2006-01-20

申请号：KR1020030025962

申请日：2003-04-24

Applicant: 강헌중

Inventor： 강헌중 ,  함정엽 ,  진정욱

IPC: C07J13/00

Abstract: 본 발명은 테스토스테론(Testosterone)으로부터 인간의 저밀도 지방단백질(LDL; low density lipoprotein) 및 콜레스테롤 수치를 효과적으로 낮추고, 고밀도 지방단백질(HDL; high density lipoprotein)을 높이는 일반식(VII)로 표시되는 4,17(20)-
E -프로스타디엔-3,16-디온(
E -Guggulsterone;
E -구굴스테론) 및 일반식(VIII)로 표시되는 4,17(20)-
Z -프로스타디엔-3,16-디온(
Z -Guggulsterone;
Z -구굴스테론)의 제조방법을 제공한다.
또한, 본 발명은 화합물 (VII) 또는 (VIII)을 제조하기 위한 중간체인 상기 일반식(IV) 및 (VI)을 합성하는 방법을 제공한다.

公开(公告)号：KR1020040092091A

公开(公告)日：2004-11-03

申请号：KR1020030025936

申请日：2003-04-24

Applicant: 강헌중

Inventor： 강헌중 ,  함정엽 ,  진정욱

IPC: C07J13/00

CPC classification number: C07J13/007 ,  A61K31/56 ,  B01J27/12 ,  B01J31/0204 ,  B01J31/0225

Abstract: PURPOSE: A process for preparing 4,17(20)-prostadien-3,16-dione from 4-androstene-3,17-dione 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 VI from 4-androstene-3,17-dione comprises the steps of: reacting 4-androstene-3,17-dione represented by formula I with an alkane dithiol under a presence of an acid catalyst; Wittig reacting it with an ethyl triphenyl phosphonium halide in an anhydrous solvent under a strong base to obtain a compound represented by formula III; de-protecting; reacting it with a selenium compound and a peroxide; and oxidizing it.

Abstract translation: 目的：提供从4-雄甾烯-3,17-二酮制备4,17（20） - 前列腺素-3,16-二酮及其制备中间体化合物的方法，用于降低低密度脂蛋白和胆固醇的含量， 增加高密度脂蛋白的值。 构成：由4-雄甾烯-3,17-二酮制备由式VI代表的4,17（20）-E-前列腺素-3,16-二酮的方法包括以下步骤：使4-雄甾烯-3,17-二酮 二醇在酸催化剂存在下用烷基二硫醇表示; Wittig在无水溶剂中在强碱下与乙基三苯基鏻卤化物反应，得到式III表示的化合物; 去保护; 与硒化合物和过氧化物反应; 并氧化它。

公开(公告)号：KR100632872B1

公开(公告)日：2006-10-16

申请号：KR1020060024792

申请日：2006-03-17

Applicant: 강헌중

Inventor： 강헌중 ,  함정엽

IPC: C07F3/02

Abstract: 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.