公开(公告)号：KR1020030086373A

公开(公告)日：2003-11-10

申请号：KR1020020024595

申请日：2002-05-04

Applicant: 강헌중 ,  함정엽

Inventor： 강헌중 ,  함정엽

IPC: C07D277/36

CPC classification number: C07C323/20 ,  C07D277/26 ,  Y02P20/55

Abstract: 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).

Abstract translation: 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。

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：KR100474202B1

公开(公告)日：2005-03-08

申请号：KR1020020024595

申请日：2002-05-04

Applicant: 강헌중 ,  함정엽

Inventor： 강헌중 ,  함정엽

IPC: C07D277/36

CPC classification number: C07C323/20 ,  C07D277/26 ,  Y02P20/55

Abstract: 본 발명은 인간의 페록시솜 증식자 활성화 수용체 δ (peroxisome proliferator activated recepter δ: hPPAR δ)형태에 활성을 갖는 일반식(X)으로 표시되는 2-{2-메틸-4-[({4-메틸-2-[4-(트리플루오로메틸)페닐]-1,3-티아졸-5-일}메틸)설파닐]펜옥시}아세트산을 하기 반응식에 따라 제조하는 방법을 제공한다.

[식중, R
1 은 탄소수 1∼4의 알킬기, 알킬 또는 아르알킬실릴 페놀 보호기를, R
2 는 수소원자와 메틸기를, R
3 는 탄소수 1∼4의 알킬기를 갖는 카르복실산 보호기를, X
1 은 할로겐 원자, 수소원자를, X
2 는 할로겐 원자 및 전자 친화반응에 반응성이 좋은 이탈기를, M은 리튬 및 마그네슘 이온를 의미한다.]
또한, 본 발명은 상기 화합물(X)을 제조하기 위한 중간체인 상기 일반식(III) 및 (VII)을 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.