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：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。