公开(公告)号：KR101075435B1

公开(公告)日：2011-10-24

申请号：KR1020090001655

申请日：2009-01-08

Applicant: 신풍제약주식회사

Inventor： 조일환 ,  이은방 ,  강신철 ,  김원석 ,  이철규

IPC: C07D239/96 ,  A61K31/517 ,  A61P25/28 ,  A61P25/08

CPC classification number: C07D403/12 ,  C07D239/96

Abstract: p는 0 또는 1의정수이다.

公开(公告)号：KR1020100057423A

公开(公告)日：2010-05-31

申请号：KR1020080116461

申请日：2008-11-21

Applicant: 신풍제약주식회사

Inventor： 김기원 ,  노정열 ,  윤지상 ,  강신철 ,  정현규 ,  주태영

IPC: A61K47/48 ,  A61K31/192 ,  A61K47/06

CPC classification number: A61K31/192 ,  A61K9/0053 ,  A61K47/02 ,  A61K47/183

Abstract: PURPOSE: A method for preparing dexibuprofen salt and a pharmaceutical composition for oral administration containing the same are provided to enhance release rate and to reduce side effect. CONSTITUTION: A method for preparing a dexibuprofen salt comprises: a step of dissolving dexibuprofen and inorganic base or organic base in two kinds of more polar solvent; a step of adding acetone to crystallize; and a step of drying crystal. The inorganic base or organic base is arginine, lysine, histidine, ornithine, NH4OH, NaOH, or KOH. A pharmaceutical composition contains the dexibuprofen salt and pharmaceutically acceptable carrier. A pharmaceutical composition for oral administration is used in the form of tablet, capsule, granule, pill, or liquid.

Abstract translation: 目的：提供一种制备右旋布洛芬盐的方法和含有这些组合物的用于口服给药的药物组合物以提高释放速率并降低副作用。 构成：一种制备右布洛芬盐的方法，其特征在于，将二苯丙酮酸和无机碱或有机碱溶解在两种极性较大的溶剂中的步骤; 加入丙酮结晶的步骤; 以及干燥晶体的步骤。 无机碱或有机碱是精氨酸，赖氨酸，组氨酸，鸟氨酸，NH 4 OH，NaOH或KOH。 药物组合物含有对映布洛芬盐和药学上可接受的载体。 用于口服给药的药物组合物以片剂，胶囊剂，颗粒剂，丸剂或液体的形式使用。

公开(公告)号：KR1020090083848A

公开(公告)日：2009-08-04

申请号：KR1020090001655

申请日：2009-01-08

Applicant: 신풍제약주식회사

Inventor： 조일환 ,  이은방 ,  강신철 ,  김원석 ,  이철규

IPC: C07D239/96 ,  A61K31/517 ,  A61P25/28 ,  A61P25/08

CPC classification number: C07D403/12 ,  C07D239/96

Abstract: A novel quinazoline-2,4-dione derivative is provided to have the effects of antioxidation, anticonvulzure, and vasorelaxant and enhance memory and prevent and treat stroke, neurodegenerative disease, Alzheimer disease and epilepsia. A method for manufacturing quinazoline-2,4-dione compound of the chemical formula (I) comprises: a step of reacting a compound of the chemical formula (IV) with amine compound of the chemical formula (V) to obtain a compound of the chemical formula (IX); or a step of reacting a first amine compound of the chemical formula (VI) with compound of the chemical formula (VII) or (VIII) to obtain the compound of the chemical formula (IX); a step of substituting a second amine compound of the chemical formula (IX) with R2, R3 or R2 and R3 to obtain a compound of the chemical formula (Ia); and a step of removing protection group. The compound of the chemical formula (IV) is an ethyl 2-ethoxycarbonylamino benzoate.

Abstract translation: 提供了一种新颖的喹唑啉-2,4-二酮衍生物，具有抗氧化，抗痉挛和血管舒张作用，增强记忆力，预防和治疗中风，神经退行性疾病，阿尔茨海默病和癫痫。 化学式（I）的喹唑啉-2,4-二酮化合物的制造方法包括：使化学式（IV）的化合物与化学式（V）的胺化合物反应的步骤，得到化合物 化学式（IX）; 或使化学式（VI）的第一种胺化合物与化学式（VII）或（VIII）的化合物反应以获得化学式（IX）的化合物的步骤; 用R2，R3或R2和R3取代化学式（IX）的第二种胺化合物以获得化学式（Ia）的化合物的步骤; 并删除保护组的一个步骤。 化学式（IV）的化合物是2-乙氧基羰基氨基苯甲酸乙酯。

公开(公告)号：KR100354271B1

公开(公告)日：2002-09-28

申请号：KR1020000005071

申请日：2000-02-02

Applicant: 신풍제약주식회사

Inventor： 한신 ,  박우일 ,  강신철

IPC: C07C229/00

Abstract: 본 발명은 해열제, 골관절염 및 류마티스관절염 등의 관절질환과 각종 통증에 우수한 치료 효과를 나타내는 소염진통제로 널리 알려져 있는 화학식 1의 화합물[관용명:아세클로페낙(Aceclofenac)]의 신규 제조방법 및 그 제조 과정에서 중간체로 사용되는 화학식 2의 화합물 및 그의 제조방법에 관한 것이다:


상기식에서, R
1 은 C
1-4 알킬렌이고 R
2 는 C
1-4 알킬이다.
본 발명은 매우 저렴하고 사용이 편리한 산(acid)을 사용하여 선택적으로 가수분해시킴으로써 고수율 및 고순도의 화학식 1의 아세클로페낙을 간편하게 제조할 수 있다.

公开(公告)号：KR100699457B1

公开(公告)日：2007-03-27

申请号：KR1020050066421

申请日：2005-07-21

Applicant: 신풍제약주식회사

Inventor： 김기원 ,  박우일 ,  강신철 ,  김영배 ,  이승규 ,  김덕훈

IPC: C07D337/14

Abstract: 본 발명은 약학적 활성을 가지는 하기의 구조식 I의 화합물 2-(10,11-디히드로-10-옥소벤조[
b,f ]티에핀-2-일)프로피온산(이하, '구조식 I의 디벤조티에핀 유도체'라 칭한다) 및 그 중간체인 하기의 구조식 IV의 고리화된 할로케톤 화합물의 제조방법에 관한 것이다:


상기 식에서 X는 할로겐원자이다.
본 발명의 제조방법에 따르면 종래 방법에 비해 간단한 방법으로 약학적 활성을 가지는 구조식 I의 디벤조티에핀 유도체를 고순도 및 고수율로 제조할 수 있다.
디벤조티에핀 유도체, 소염진통작용, 고리화반응, 제조 수율

公开(公告)号：KR1020070011824A

公开(公告)日：2007-01-25

申请号：KR1020050066421

申请日：2005-07-21

Applicant: 신풍제약주식회사

Inventor： 김기원 ,  박우일 ,  강신철 ,  김영배 ,  이승규 ,  김덕훈

IPC: C07D337/14

Abstract: A method for preparing a dibenzothiepin derivative is provided to obtain the pharmaceutically active dibenzothiepin derivative with high purity and high yield through a simple process. The method for preparing a dibenzothiepin derivative represented by the formula(I) comprises the steps of: (a) reacting a propiophenone represented by the formula(II) with a halogenating agent to obtain a halo-ketone compound represented by the formula(III); (b) reacting the compound(III) with a condensing agent to obtain a cyclized halo-ketone compound represented by the formula(IV); (c) reacting the compound(IV) with an alkylorthoformate to obtain a cyclized haloacetal represented by the formula(V); (d) reacting the compound(V) with a zinc halide to obtain an ester compound represented by the formula(VI); and (e) hydrolyzing the compound(VI) to prepare the compound(I). In the formulae, X is halogen, and R1 is C1-6 alkyl, phenyl or phenyl having a substituent selected from the group consisting of H, halogen, C1-6 alkyl, and hydroxy.

Abstract translation: 提供了制备二苯并硫代衍生物的方法，以通过简单的方法获得高纯度和高产率的药物活性二苯并硫代衍生物。 制备由式（I）表示的二苯并硫代衍生物的方法包括以下步骤：（a）使由式（II）表示的苯丙酮酮与卤化剂反应，得到由式（III）表示的卤代酮化合物， ; （b）使化合物（III）与缩合剂反应，得到式（IV）所示的环化的卤代酮化合物; （c）使化合物（Ⅳ）与原甲酸烷基酯反应得到由式（Ⅴ）表示的环化的卤代缩醛; （d）使化合物（V）与卤化锌反应，得到式（VI）表示的酯化合物; 和（e）水解化合物（VI）以制备化合物（I）。 在该式中，X是卤素，R 1是C 1-6烷基，苯基或具有选自H，卤素，C 1-6烷基和羟基的取代基的苯基。

公开(公告)号：KR1020010077337A

公开(公告)日：2001-08-17

申请号：KR1020000005071

申请日：2000-02-02

Applicant: 신풍제약주식회사

Inventor： 한신 ,  박우일 ,  강신철

IPC: C07C229/00

Abstract: PURPOSE: An intermediate for preparing £2-(2,6-dichloroanilino)phenyl| acetoxyacetic acid (referred as "aceclofenac") used as an anti-inflammatory and analgesic agent, and methods for preparing aceclofenac are provided to improve production yield and purity without a process of waste heavy metal. CONSTITUTION: The intermediate which is used for preparing aceclofenac represented by the formula 1, is represented by the formula 2, wherein R1 and R2 are independent of each other and are an alkyl group of C1-C4. Aceclofenac is prepared by selectively hydrolyzing the intermediate of the formula 2 by using an acid in organic solvent. Preferably, the acid is HCl, H2SO4 or methanesulfonic acid; the solvent is alkyl acetate of C1-C5; and the reaction temperature is 20-40 deg.C. The intermediate of the formula 2 is prepared by reacting the alkali metal salt of compound of the formula 3 with the compound of the formula 4(X-CH2-COO-CH2OR¬1OR¬2) in solvent, wherein R1 and R2 are independent each other and are an alkyl group of C1-C4, and X is a halogen atom. Preferably X is Cl or Br; and the solvent is DMF or DMSO.

Abstract translation: 目的：制备2-（2,6-二氯苯胺基）苯基的中间体 用作抗炎和止痛剂的乙酰氧基乙酸（称为“醋氯芬酸”），以及制备醋氯芬酸的方法，以提高生产产率和纯度，而无需重金属废物。 构成：用于制备由式1表示的醋氯芬酸的中间体由式2表示，其中R 1和R 2彼此独立并且是C 1 -C 4的烷基。 通过在有机溶剂中使用酸选择性水解式2的中间体来制备醋氯芬酸。 优选地，酸是HCl，H 2 SO 4或甲磺酸; 溶剂是C1-C5的烷基乙酸酯; 反应温度为20-40℃。 式2的中间体通过使式3的化合物的碱金属盐与式4的化合物（X-CH 2 -COO-CH 2 OR 1 OR 2）在溶剂中反应制备，其中R 1和R 2各自独立地 另外是C1-C4的烷基，X是卤素原子。 优选地，X是Cl或Br; 溶剂为DMF或DMSO。