公开(公告)号：KR100530345B1

公开(公告)日：2005-11-22

申请号：KR1020020066652

申请日：2002-10-30

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  장문호 ,  고훈영 ,  배애님 ,  전보경

IPC: C07C209/32

Abstract: 본 발명은 인듐 금속 와이어를 사용하여 아래의 화학식 1로 표시되는 니트로 화합물을 상온 및 수용액 중에서 화학식 2로 표시되는 아민 화합물로 환원시키는 방법에 관한 것으로서, 식 중, R은 지방족 또는 방향족 화합물을 나타낸다.
[화학식 1]

[화학식 2]

公开(公告)号：KR1020040083677A

公开(公告)日：2004-10-06

申请号：KR1020030018239

申请日：2003-03-24

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  장문호 ,  고훈영 ,  배애님 ,  차주환 ,  전보경

IPC: C07C17/272

Abstract: PURPOSE: Provided is a method for preparing various types of 2-halo-1,3-diene compounds from allenol with ease by a simple process using no catalyst at a high yield. CONSTITUTION: The method for preparing a 2-halo-1,3-diene represented by formula 3 from an allenol represented by formula 2 comprises treating the allenol with an indium(III) halide salt represented by the formula of InX3 (wherein X is Cl, Br or I), through the reaction route as depicted in the following formula 4. In formulas 2 to 4, each of R1 to R4 represents H, Si, a halogen atom, an alkyl group, an aromatic substituent or a cyclic substituent. In the method, the reaction solvent is selected from acetonitrile and benzene.

Abstract translation: 目的：提供一种通过简单的方法，以高收率使用不含催化剂的方法从丙烯醇制备各种类型的2-卤代-1,3-二烯化合物。 构成：由式2由式2表示的联苯酚制备由式3表示的2-卤代-1,3-二烯的方法包括用式InX 3（其中X为Cl）表示的卤化铟（III）处理三烯酚 ，Br或I）通过如下式4所示的反应路线。在式2至4中，R 1至R 4各自表示H，Si，卤素原子，烷基，芳族取代基或环状取代基。 在该方法中，反应溶剂选自乙腈和苯。

公开(公告)号：KR100451413B1

公开(公告)日：2004-10-06

申请号：KR1020010087362

申请日：2001-12-28

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  최경일 ,  조용서 ,  배애님 ,  차주환 ,  한예선 ,  이종수 ,  윤홍철

IPC: C07D209/48

CPC classification number: C07D209/48

Abstract: A compound represented by a general formula (Ia) or (Ib) and a stereo-selective preparation method thereof using a carbonyl reductase which is separated from Kluyveromyces marxianus. The compound can be prepared by reduction of substituted beta-keto ester and can be used as an intermediate in preparing beta-lactam group antibiotics.

Abstract translation: 由通式（Ia）或（Ib）表示的化合物及其立体选择性制备方法，其使用从马克斯克鲁维酵母分离的羰基还原酶。 该化合物可以通过还原取代的β-酮酯来制备，并且可以用作制备β-内酰胺类抗生素的中间体。

公开(公告)号：KR100448002B1

公开(公告)日：2004-09-13

申请号：KR1020020005946

申请日：2002-02-01

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  최경일 ,  조용서 ,  배애님 ,  차주환 ,  석미영 ,  공재양 ,  정대영

IPC: C07D453/02

Abstract: PURPOSE: Provided are Quinuclidine compounds which are useful for treatment of brain-nervous diseases caused by cholinergic neurotransmission such as Alzheimer's disease and a preparation method thereof. CONSTITUTION: A quinuclidine compounds of the formula (I) and pharmaceutically acceptable salts thereof are provided, wherein n is an integer of 1 to 5; R is a substituent on a benzene ring, hydrogen, F, Cl, methoxy, OH, NH2, NO2, 3,4-dimethoxy, 2,4-dimethoxy, cyano, C1-6 alkyl, 1,2 or 3 fluorine substituted C1-6 alkyl, 4-methoxybenzyloxy, t-butoxycarbonyl, C2-6 alkenyl, 1,2 or 3 fluorine substituted C2-6 alkenyl, C2-6 alkynyl, 1,2 or 3 fluorine substituted C2-6 alkynyl, and C3-7 cycloalkyl. A method for preparing the quinuclidine compounds of the formula (I) comprises reacting a compound of the formula (II) with a compound of the formula (III) or (IV), wherein R1 and R2 are independently C1-6 alkyl, aryl or arylalkyl.

Abstract translation: 目的：提供用于治疗由胆碱能神经传递引起的脑神经疾病如阿尔茨海默氏病的奎宁环化合物及其制备方法。 构成：提供式（I）的奎宁环化合物及其药学上可接受的盐，其中n是1至5的整数; R为苯环上的取代基，氢，F，Cl，甲氧基，OH，NH2，NO2,3,4-二甲氧基，2,4-二甲氧基，氰基，C1-6烷基，1,2或3个氟取代的C1 -6烷基，4-甲氧基苄氧基，叔丁氧基羰基，C2-6烯基，1,2或3个氟取代的C2-6烯基，C2-6炔基，1,2或3个氟取代的C2-6炔基和C3-7 环。 用于制备式（I）奎宁环化合物的方法包括使式（II）化合物与式（III）或（IV）化合物反应，其中R 1和R 2独立地为C 1-6烷基，芳基或 芳。

公开(公告)号：KR100418915B1

公开(公告)日：2004-02-14

申请号：KR1020000071399

申请日：2000-11-28

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  조용서 ,  최경일 ,  배애님 ,  강경호 ,  이희윤 ,  손정훈 ,  공재양 ,  정대영

IPC: C07D401/04

Abstract: PURPOSE: A 4-aminopiperidine analogue and a producing method thereof are provided, therefore the compound can be useful as a ligand of a muscarine receptor, and it is thus used in study on Alzheimer disease. CONSTITUTION: The 4-aminopiperidine analogue is represented by formula(I), wherein R1, R2, R3, R4, R5, R6 and R7 are hydrogen, cycloalkyl having carbon number of 1 to 6, alkoxy, halogen, hydroxy, hydroxymethyl, aryl, heteroaryl, amino, alkylamino, alkenyl, carbonyl or hetero ring having carbon number of 5 to 7 wherein aryl is a ring having 6 atoms, two rings having 10 atoms or a stable resonance form having double bond to adjacent carbon; heteroaryl is a single ring aromatic group having carbon number of 5 to 6 or a double ring aromatic group having carbon number of 10 in which the heteroaryl has at least one hetero atom of N, O or S; hetero ring consists of 5 to 7 atoms having 1 to 3 of N, O or S; X is carbon or sulfur; and n is an integer of 1 to 2 wherein n is 1 when X is carbon and is 2 when X is sulfur. The 4-aminopiperidine analogue is produced by reacting piperidine or amine(II) with piperazine with ketone(III) in the presence of 1 to 3 equivalent of acetic acid, 2 to 10 equivalent of reducing agent and solvent at room temperature for 3 to 24 hours to produce 4-aminopiperidine(I) and adding NaHCO3 solution and organic solvent to 4-aminopiperidine(I); and drying the extracted 4-aminopiperidine(I), dissolving it, adding 1 to 10 equivalent of hydrogen chloride to the solution, and separating, washing and drying the hydrochloride of 4-aminopiperidine.

Abstract translation: 目的：提供了4-氨基哌啶类似物及其生产方法，因此该化合物可用作毒蕈碱受体的配体，因此用于研究阿尔茨海默病。 构成：4-氨基哌啶类似物由式（I）表示，其中R1，R2，R3，R4，R5，R6和R7是氢，碳数为1-6的环烷基，烷氧基，卤素，羟基，羟甲基，芳基 杂芳基，氨基，烷基氨基，链烯基，羰基或杂环，其中芳基是具有6个原子的环，具有10个原子的两个环或具有与相邻碳双键的稳定的共振形式; 杂芳基为碳数为5至6的单环芳族基团或碳数为10的双环芳族基团，其中杂芳基具有至少一个N，O或S的杂原子; 杂环由5至7个具有1至3个N，O或S的原子组成; X是碳或硫; 并且n是1至2的整数，其中当X是碳时，n是1，当X是硫时，n是2。 4-氨基哌啶类似物是通过使哌啶或胺（II）与哌嗪与酮（III）在1至3当量乙酸，2至10当量还原剂和溶剂的存在下在室温下反应3至24 小时以产生4-氨基哌啶（I）并将NaHCO 3溶液和有机溶剂加入到4-氨基哌啶（I）中; 干燥提取的4-氨基哌啶（I），溶解，加入1至10当量的氯化氢至溶液中，分离，洗涤并干燥4-氨基哌啶的盐酸盐。

公开(公告)号：KR100394083B1

公开(公告)日：2003-08-06

申请号：KR1020000073122

申请日：2000-12-04

Applicant: 한국과학기술연구원 ,  한국과학기술원 ,  한국화학연구원 ,  학교법인 성신학원

Inventor： 고훈영 ,  최경일 ,  조용서 ,  배애님 ,  공재양 ,  정대영 ,  정선호 ,  정지영 ,  이희윤

IPC: C07D413/14

CPC classification number: C07D413/04 ,  C07D261/08

Abstract: The present invention relates to 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 and D4 receptors represented by the following Formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent,wherein R1, R2, X and n are the same as defined in the specification.

Abstract translation: 本发明涉及对下式（1）所示的多巴胺D3和D4受体具有选择性生物活性的4,5-二氢异恶唑烷基哌嗪衍生物及其在还原剂存在下通过还原胺化反应的制备方法，其中R1，R2， X和n与说明书中定义的相同。

公开(公告)号：KR1020030064159A

公开(公告)日：2003-07-31

申请号：KR1020020004657

申请日：2002-01-26

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  한예선 ,  차주환 ,  김욱현 ,  이종수 ,  윤홍철

IPC: C12N9/02

CPC classification number: C12N9/0006

Abstract: PURPOSE: A carbonyl reductase of Kluyveromyces marxianus and an isolation and purification method thereof are provided, thereby higher stereo-selectively, cheaply and rapidly carrying out the reduction process. CONSTITUTION: A carbonyl reductase isolated and purified from Kluyveromyces marxianus has the properties of the size of 40 to 42 kDa, the active temperature of 25 to 35 deg. C, and the active pH of 6.5 to 7.5, wherein the carbonyl reductase contains the amino acid sequence of Thr-Phe-Thr-Val-Val-Thr-Gly in the amino-terminal. A method for isolating and purifying the carbonyl reductase of Kluyveromyces marxianus comprises the steps of: (1) culturing Kluyveromyces marxianus; (2) centrifuging the cultured medium to collect the pellet and pulverizing the pellet; and (3) centrifuging the pulverized cell extract to collect the supernatant, and subjecting the supernatant to column chromatography to isolate an active fraction containing active material to substrate, wherein the column uses Q sepharose, phenyl sepharose, high-trap blue and gel filtration chromatography, sequentially.

Abstract translation: 目的：提供马克斯克鲁维酵母的羰基还原酶及其分离和纯化方法，从而立体选择性更好，成本低廉且快速地进行还原过程。 构成：从马克斯克鲁维酵母分离和纯化的羰基还原酶具有40至42kDa大小的性质，活性温度为25至35度。 C，活性pH为6.5〜7.5，其中羰基还原酶含有氨基末端的Thr-Phe-Thr-Val-Val-Thr-Gly的氨基酸序列。 分离和纯化马克斯克鲁维酵母的羰基还原酶的方法包括以下步骤：（1）培养马克斯克鲁维酵母; （2）离心培养基以收集颗粒并粉碎颗粒; （3）将粉碎的细胞提取物离心以收集上清液，并将上清液进行柱色谱以将含有活性物质的活性级分与底物分离，其中该柱使用Q琼脂糖凝胶，苯基琼脂糖凝胶，高陷阱蓝和凝胶过滤色谱 ，顺序。

公开(公告)号：KR1020030063853A

公开(公告)日：2003-07-31

申请号：KR1020020004199

申请日：2002-01-24

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  최경일 ,  조용서 ,  배애님 ,  차주환 ,  공재양 ,  정대영

IPC: C07D453/02 ,  C07D471/08 ,  C07D261/06

Abstract: PURPOSE: An alkenyl azabicyclic compound and a preparation method thereof are provided, which can be useful for treatment of cerebral nervous diseases caused by choline neurotransmission disorders. CONSTITUTION: An alkenyl azabicyclic compound represented by the formula(I) and pharmaceutically acceptable salts thereof are provided, wherein n is 1 or 2; and R is selected from the group consisting of hydrogen, F, Cl, methoxy, OH, NH2, NO2, 3,4-dimethoxy, 2,4-dimethoxy, cyano, C1-C6 alkyl, 1, 2 or 3 fluorine substituted C1-C6 alkyl, 4-methoxybenzyloxy, t-butoxycarbonyl, C2-C6 alkenyl, 1, 2 or 3 fluorine substituted C2-C6 alkynyl and C3-C7 cyloalkyl. A method for preparing the alkenyl azabicyclic compound of the formula(I) comprises a compound of the formula(II) with a compound of the formula(III) or formula(IV), wherein R1, R2 and R3 are independently C1-C6 alkyl, aryl or arylalkyl.

Abstract translation: 目的：提供一种烯基氮杂双环化合物及其制备方法，其可用于治疗由胆碱神经传递障碍引起的脑神经疾病。 构成：提供由式（I）表示的烯基氮杂双环化合物及其药学上可接受的盐，其中n为1或2; 并且R选自氢，F，Cl，甲氧基，OH，NH 2，NO 2，3,4-二甲氧基，2,4-二甲氧基，氰基，C 1 -C 6烷基，1,2或3个氟取代的C 1 C 1-6烷基，4-甲氧基苄氧基，叔丁氧基羰基，C 2 -C 6烯基，1,2或3个氟取代的C 2 -C 6炔基和C 3 -C 7环烷基。 制备式（I）的烯基氮杂双环化合物的方法包括式（II）化合物与式（III）或式（IV）化合物，其中R 1，R 2和R 3独立地为C 1 -C 6烷基 ，芳基或芳烷基。

公开(公告)号：KR1020000074954A

公开(公告)日：2000-12-15

申请号：KR1019990019241

申请日：1999-05-27

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  장문호 ,  조영서 ,  최경일 ,  배애님 ,  김혜연 ,  주현진

IPC: C07D413/14

Abstract: PURPOSE: Provided is an isooxazolyl methylene oxazolidinone derivative represented by the formula (I) which is superior in antibacterial activity. Also, a method for preparing the compound is provided. CONSTITUTION: An isooxazoly methylene oxazolidinone derivative is represented by the formula (I): wherein, R is hydrogen, alkyl, halogen such as bromine or chlorine, cyano, alkoxy, hydroxy, carboxy, carbamoyl, N,N'-dimethylcarbamoyl, carbamoyloxy, oxygen, sulfur, thiopene having more than one nitrogen atom, thiazole, aminothiazole, isothiazole, isooxazole, oxazole, tetrazole, 5 or 6-membered unsaturated heterocycle substituent of pyridine, alkyl, halogenalkoxy, benzene ring substituted with cyano or phenoxy group, pharmaceutically acceptable methanesulfonate, fumarate, bromate, citrate, phosphate, sulfate or amine not being salt. The isooxazoly methylene oxazolidinone derivative is prepared by reacting oxazolidine derivative represented by the formula (II) and isooxazole derivative represented by the formula (III) a using a reductant in the presence of a solvent.

Abstract translation: 目的：提供抗菌活性优异的由式（I）表示的异恶唑基亚甲基恶唑烷酮衍生物。 此外，提供了制备该化合物的方法。 构型：异恶唑基亚甲基恶唑烷酮衍生物由式（I）表示：其中R是氢，烷基，卤素如溴或氯，氰基，烷氧基，羟基，羧基，氨基甲酰基，N，N'-二甲基氨基甲酰基，氨基甲酰氧基， 氧，硫，具有多于一个氮原子的噻吩，噻唑，氨基噻唑，异噻唑，异恶唑，恶唑，四唑，吡啶，烷基，卤代烷氧基，被氰基或苯氧基取代的苯环的5或6元不饱和杂环取代基， 甲磺酸盐，富马酸盐，溴酸盐，柠檬酸盐，磷酸盐，硫酸盐或胺不是盐。 异恶唑亚甲基恶唑烷酮衍生物通过使用还原剂在溶剂存在下使式（II）表示的恶唑烷衍生物和由式（III）a表示的异恶唑衍生物反应来制备。

公开(公告)号：KR1020000073204A

公开(公告)日：2000-12-05

申请号：KR1019990016354

申请日：1999-05-07

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  최경일 ,  배애님 ,  고훈영 ,  장문호 ,  김유승 ,  이지은

IPC: C07D499/00

CPC classification number: Y02P20/55

Abstract: PURPOSE: A new penam derivative using indium and zinc and a preparation method thereof are provided CONSTITUTION: A novel penam derivative represented by formula(I) is prepared by reacting 6-oxopenam of the formula(I') with ally halide of the formula (II) or acetylene halide of the formula (III) in the presence of indium or zinc. In the formula(I): R1 is allyl derivative and acetylene derivative; R2 is hydrogen, carboxylic acid salt(sodium salt and potassium salt as inorganic salt, alkyl amine salt, aromatic amine salt as organic salt) or carboxy protecting group(4-methoxy benzyl, diphenylmethyl, 4-nitrobenzyl, useful thing as protecting group of molecule in penicillin or cephalosporin compound field); R3 is hydrogen, halogen, hydroxy, acetoxy group.

Abstract translation: 目的：提供使用铟和锌的新的penam衍生物及其制备方法构成：式（I）表示的新型penam衍生物通过式（I'）的6-氧代青霉素与式（I'）的式 II）或式（III）的炔酰卤在铟或锌的存在下进行。 在式（I）中：R 1是烯丙基衍生物和乙炔衍生物; R2为氢，羧酸盐（钠盐和钾盐为无机盐，烷基胺盐，芳族胺盐为有机盐）或羧基保护基（4-甲氧基苄基，二苯基甲基，4-硝基苄基，有用物质为保护基 分子在青霉素或头孢菌素化合物领域）; R3是氢，卤素，羟基，乙酰氧基。