公开(公告)号：KR100343947B1

公开(公告)日：2002-07-22

申请号：KR1019990041613

申请日：1999-09-28

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  조용서 ,  최경일 ,  배애님 ,  강경호 ,  이지은 ,  이희윤 ,  공재양 ,  정대영 ,  정선호

IPC: C07D413/06

Abstract: 본발명은화학식 1을갖는이소옥사졸피페라진계열의화합물또는그 염의제조방법및 상기방법에의해만들어진라이브러리에관한것으로, 상기방법은화학식 2의화합물과화학식 3의화합물을염기및 염소화제의존재하에 1,3-쌍극자고리화첨가반응시켜화학식 1 또는그 염의화합물을제조하는것으로구성된다. 그화학식 1, 2, 3과반응식 1은다음과같다. 상기화학식 1, 2, 3과반응식 1에서, R및 R는페닐, 벤질, 할로겐화페닐, C-C의알킬기로치환된페닐, C-C의알콕시기로치환된페닐, (트리플루오로)메틸페닐, 피리딜등의페닐유도체를말하며, R-R는수소이며, X는질소이며,는이중결합또는삼중결합을의미하며,는이중결합또는단일결합을의미한다.

公开(公告)号：KR1020020043413A

公开(公告)日：2002-06-10

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: PURPOSE: Provided are novel 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity to dopamine D3 and D4 receptors, and their preparation method by reductive amination in the presence of reductant. CONSTITUTION: 4,5-dihydroisoxazolylalkylpiperazine derivative is represented by the formula(1), wherein R1, R2, R3, R4 and R5 are identical or different from each other, and represents individually hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 alkoxy group, C2-C6 alkenyl group, hydroxy group , hydroxymethyl group, aryl group, heteroaryl group, amino group, C1-C6 alkyl amino group, carbonyl group, C3-C8 cycloalkyl group, or C3-C8 heterocyclic group; R6 represents hydrogen atom, halogen atom, alkyl group, C1-C6 alkoxy group, aryl group, pyridyl group, heterocyclic group or pyrimidyl group; X represents CH or nitrogen atom; and n is 3 or 4.

Abstract translation: 目的：提供对多巴胺D3和D4受体具有选择性生物活性的新型4,5-二氢异恶唑烷基哌嗪衍生物及其在还原剂存在下还原胺化的制备方法。 构成：4,5-二氢异恶唑基烷基哌嗪衍生物由式（1）表示，其中R 1，R 2，R 3，R 4和R 5彼此相同或不同，并且表示单独的氢原子，卤素原子，C1-C6烷基， C1-C6烷氧基，C2-C6烯基，羟基，羟甲基，芳基，杂芳基，氨基，C1-C6烷基氨基，羰基，C3-C8环烷基或C3-C8杂环基; R6表示氢原子，卤素原子，烷基，C1-C6烷氧基，芳基，吡啶基，杂环基或嘧啶基; X表示CH或氮原子; n为3或4。

公开(公告)号：KR100333493B1

公开(公告)日：2002-04-25

申请号：KR1019990019242

申请日：1999-05-27

Applicant: 한국과학기술연구원

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

IPC: C07D413/14

Abstract: 일반식(II)로표시되는옥사졸리디논유도체와일반식(III)으로표시되는카르복실산유도체를활성화제, 염기및 용매존재하에아실화반응시켜 MRSA 균주를포함한그람양성균에우수한신규의일반식 (I)로표시되는이소옥사졸릴카르보닐옥사졸리디논유도체및 이의제조방법에관한것이다. 상기식들중, R은수소, 알킬, 브롬또는염소의할로겐, 시아노, 알콕시, 히드록시, 카르복시, 카르바모일, N,N'-디메틸카르바모일, 카르바모일옥시, 산소, 황, 질소원자를적어도한 개이상포함하고있는티오펜, 티아졸, 티아디아졸, 아미노티아졸, 이소티아졸, 이소옥사졸, 옥사졸, 옥사디아졸, 테트라졸, 피리딘의불포화 5환또는 6환헤테로고리치환체, 알킬, 할로겐, 알콕시, 시아노또는페녹시가치환된벤젠고리치환체, 약제학적으로허용되는염의메탄설폰산염, 퓨마렌산염, 브롬산염, 시트릭산염, 말레인산염, 인산염, 황산염, 나트륨염, 염산염또는염이아닌아민을포함한다.

公开(公告)号：KR100264156B1

公开(公告)日：2001-11-22

申请号：KR1019980002915

申请日：1998-02-03

Applicant: 한국과학기술연구원

Inventor： 김중협 ,  장문호 ,  김유승 ,  고훈영 ,  김성훈 ,  최경일 ,  배애님 ,  강순방 ,  구창휘 ,  문종택

IPC: C07D501/24

Abstract: PURPOSE: Provided is (E)-prophenyl quaternary ammonium cephem compound and a pharmaceutically acceptable salt and a method for preparation thereof. The prepared compound has excellent antibacterial activity against both gram positive and gram negative strains, and is thus used for Cephalosporin based medicines. CONSTITUTION: (E)-prophenyl quaternary ammonium cephem compound is represented by the formula(1), wherein R1 is hydrogen, formyl, t-buthoxycarbonyl, benzyloxycarbonyl, p-nitrobenzyloxycarbonyl or trithyl; R2 is hydrogen, methyl, 2-fluoroethyl, formyl, chloroacetyl, benzoyl, p-nitrobenzyl, 2,2,2-trichloroethoxycarbonly, tetrahydropyranyl or trithyl; R3 is hydrogen, group forming carboxylic salt, 2,2,2-trichloroethyl, p-methoxybenzyl, p-nitrobenzyl, benzhydryl or t-butyl; R4 is methoxy, carbamoyl having substituent, or C5 hetero ring substituent represented by oxydiazole or triazole; and n is an integer of 1 or 2.

公开(公告)号：KR1020010097299A

公开(公告)日：2001-11-08

申请号：KR1020000021258

申请日：2000-04-21

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  김유승 ,  고훈영 ,  최경일 ,  배애님 ,  이정규

IPC: C07C209/32

Abstract: 본 발명은 인듐 금속을 이용하여 니트로기(-NO
2 )를 갖는 화합물을 아민(-NH
2 ) 화합물로 환원시키는 방법을 제공한다. 보다 구체적으로는 인듐 금속을 이용하여 화학식 1을 갖는 지방족 또는 방향족 화합물을 화학식 2의 화합물로 환원시키는 방법을 제공한다.
[화학식 1]

[화학식 2]

상기 화학식 1 및 2에서, R은 지방족 또는 방향족 화합물을 나타내며, n은 1-5의 정수, 바람직하게는 1-3의 정수, 가장 바람직하게는 1 또는 2이다.
인듐 금속을 이용한 본 발명의 환원 반응은 상온에서 짧은 시간 내에 진행될 뿐만 아니라 수개의 니트로기를 짧은 시간 내에 한번에 환원시킬 수 있다. 또한 분자내 다른 관능기에 영향을 미치지 아니하고 니트로기만 선택적으로 환원시킬 수 있으며, 수용액 상에서 반응이 쉽게 진행되므로 환경친화적 산업 공정이다는 장점을 가지고 있다. 따라서 화학 공업 분야에서 다양하게 응용될 수 있다.

公开(公告)号：KR1020010046869A

公开(公告)日：2001-06-15

申请号：KR1019990050824

申请日：1999-11-16

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  조용서 ,  최경일 ,  배애님 ,  강경호 ,  이희윤

IPC: C07D403/02

Abstract: PURPOSE: The piperazinylethyl triazole derivatives and a producing method thereof are provided, thereby the piperazinylethyl triazole compounds can be produced in higher yield and purity. CONSTITUTION: The piperazinylethyl triazole derivatives are represented by formula (1), in which R1 is C6 to C10 aromatics, C6 to C10 aromatic carbohydrate substituted with C1 to C6 alkyl, C6 to C10 aromatic carbohydrate substituted with C1 to C4 alkoxy, C6 to C10 aromatic carbohydrate substituted with halogen or C7 to C10 arylalkyl; R2 to R5 are independently hydrogen, halogen, methyl or ethyl; R6 to R7 are independently hydrogen, phenoxy substituted with halogen, -OC(O)R8 or -NR9R10; Y is O or S; R8 is C1 to C6 alkyl; R9 and R10 is independently C1 to C6 alkyl; R11 is hydrogen, C1 to C6 alkyl or phenyl; R12 is independently hydrogen or C1 to C6 alkyl; n is an integer of 1 or 2; k is 5 or 6 when n is 1 or 2, respectively; and m is 4 or 5 when n is 1 or 2, respectively. The piperazinylethyl triazole derivatives is produced by separation and purification using acid.

Abstract translation: 目的：提供哌嗪基乙基三唑衍生物及其制备方法，从而可以更高的产率和纯度制备哌嗪基乙基三唑化合物。 构成：哌嗪基乙基三唑衍生物由式（1）表示，其中R1为C6至C10芳族化合物，C6至C10芳族碳水化合物被C1至C6烷基取代，C6至C10芳族碳水化合物被C1至C4烷氧基取代，C6至C10 用卤素或C 7至C 10芳基烷基取代的芳族碳水化合物; R2至R5独立地为氢，卤素，甲基或乙基; R6至R7独立地为氢，被卤素取代的苯氧基，-OC（O）R8或-NR9R10; Y为O或S; R8是C1-C6烷基; R9和R10独立地为C1至C6烷基; R11是氢，C1-C6烷基或苯基; R 12独立地为氢或C 1至C 6烷基; n是1或2的整数; 当n分别为1或2时，k为5或6; 当n分别为1或2时，m为4或5。 哌嗪基乙基三唑衍生物通过使用酸的分离和纯化而产生。

公开(公告)号：KR1020010046868A

公开(公告)日：2001-06-15

申请号：KR1019990050823

申请日：1999-11-16

Applicant: 한국과학기술연구원

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

IPC: C07D261/14

Abstract: PURPOSE: A novel tertiary aminoethyl isooxazol derivative is provided, which acts as an antagonist of dopamine-1 receptor relating to various central nervous system disorders. And a method for preparing the same is also provided. CONSTITUTION: The tertiary aminoethyl isooxazol derivative is represented by the formula (1) and is prepared by dissolving a compound represented by the formula (2) and a compound represented by the formula (3) in a solvent to react them with each other in the presence of base. In the formulae 1-3, R1 is phenyl, phenyl substituted by halogen atom, phenyl substituted by trifluoromethyl, phenyl methyl having a trifluoromethyl substituent in 2, 3 or 4 position of the phenyl group, diphenylmethyl having a halogen atom substituent in 2, 3 or 4 position of the phenyl group, benzyl or 3-hydrobenzimidazole-2-one, each R2-R5 is hydrogen, R6 is phenyl substituted by at least one selected from the group consisting of nitro group, phynoxy group, methoxy group, trifluoromethyl group and halogen group, vinyl substituted by phenyl group or C5 or C6 unsaturated or saturated hetero cyclic compound substituted by O, S or N, and X is nitrogen or carbon.

Abstract translation: 目的：提供一种新的叔氨基乙基异恶唑衍生物，其作为与各种中枢神经系统疾病有关的多巴胺-1受体的拮抗剂。 还提供了制备该方法。 构成：叔氨基乙基异恶唑衍生物由式（1）表示，通过将式（2）表示的化合物和式（3）表示的化合物溶解在溶剂中，使其在 存在基地 式1-3中，R 1为苯基，被卤素原子取代的苯基，被三氟甲基取代的苯基，苯基2,3或4位中具有三氟甲基取代基的苯基甲基，2,3或4位的卤素原子取代基的二苯基甲基 或4位，苯基或3-氢苯并咪唑-2-酮，每个R 2 -R 5是氢，R 6是被选自硝基，环氧基，甲氧基，三氟甲基中的至少一个取代的苯基 卤素基，被苯基取代的乙烯基或被O，S或N取代的C5或C6不饱和或饱和杂环化合物，X是氮或碳。

公开(公告)号：KR1020010029024A

公开(公告)日：2001-04-06

申请号：KR1019990041612

申请日：1999-09-28

Applicant: 한국과학기술연구원

Inventor： 고훈영 ,  조용서 ,  최경일 ,  배애님 ,  강경호 ,  이희윤

IPC: C07D295/22

Abstract: PURPOSE: Provided is a novel isooxazol piperazin derivative which is used as an antagonist against dopamine-1 receptor related to the central nerve system disorders. CONSTITUTION: A novel isooxazol piperazin derivative represented by the formula (1) is manufactured by reacting secondary amine of the formula (2) with aldehyde of the formula (3) in the presence of NaBh(OAc)3, NaBH3CN, or NaBH4 as a reductant and methylene chloride as a solvent at room temperature for 3-24 hours, preferably 12-14 hours. In the formula (1), n is an integer of between 1 and 4; R1 is a phenyl group at an ortho, meta, or para position substituted by more than one group among halogen, trifluoromethyl, -NO2, alkyl group of C1-C3 , and alkoxy group of C1-C3, or an alkyl group of C1-C3, hydroxy group, 4-(2-keto-1-benzimidazolerynyl), 1-(2-(trifluoromethyl)benzene, 4-(4-chlorophenyl)-4-hydroxy, 1-(2-pyrimidyl), or 1-benzyl group; R2-R5 is hydrogen; R6 is a phenyl group at an ortho, meta, or para position substituted by more than one group among halogen group, trifluoromethyl group , -CN, -NO2, an alkyl group of C1-C3, phenoxy group, and alkoxy group of C1-C3 and an unsaturated 5 or 6 hetero ring group having more than one atom from an alkyl group of C-C3, alkoxy group of C1-C3, thiophenyl group, (2-phenyl)vinyl group, pyridyl group, and from oxygen, sulfur, and nitrogen; and Q is isoxazol (A) or 4,5-dihydroisoxazole derivative (B).

Abstract translation: 目的：提供一种新的异恶唑哌嗪衍生物，其用作与中枢神经系统疾病相关的多巴胺-1受体的拮抗剂。 构成：由式（1）表示的新型异恶唑哌嗪衍生物通过在NaBh（OAc）3，NaBH 3 CN或NaBH 4存在下，使式（2）的仲胺与式（3）的醛反应，作为 还原剂和二氯甲烷作为溶剂在室温下反应3-24小时，优选12-14小时。 在式（1）中，n为1〜4的整数， R 1是在卤素，三氟甲基，-NO 2，C 1 -C 3烷基和C 1 -C 3烷氧基中被多个基团取代的邻位，间位或对位的苯基，或C1- C3，羟基，4-（2-酮-1-苯并咪唑啉基），1-（2-（三氟甲基）苯，4-（4-氯苯基）-4-羟基，1-（2-嘧啶基） 苄基; R 2 -R 5是氢; R 6是在卤素基团，三氟甲基，-CN，-NO 2，C 1 -C 3烷基，C 1 -C 3烷基， 苯氧基，C1-C3烷氧基，C1-C3烷氧基，噻吩基，（2-苯基）乙烯基等）中具有1个以上原子的不饱和5或6个杂环基 ，吡啶基和氧，硫和氮; Q是异恶唑（A）或4,5-二氢异恶唑衍生物（B）。

公开(公告)号：KR1020000074955A

公开(公告)日：2000-12-15

申请号：KR1019990019242

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 carbonyl oxazolidinone derivative represented by the formula (I) which has an excellent antibacterial activity on gram-positive strain. Also, a preparation method of the compound is provided. CONSTITUTION: An isooxazolyl carbonyl oxazolidinone derivative represented by the formula (I) is prepared by acylation of oxazolidinone derivative of general formula (II) and carboxylic acid derivative of general formula (III) in the presence of a base and a solvent. R in the formula (II) and (III) 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, thiadiazole, aminothiazole, isothiazole, isooxazole, oxazole, oxadiazole, tetrazole, 5 or 6-membered unsaturated heterocycle substituent of pyridine, alkyl, halogen, alkoxy, benzene ring substituted with cyano or phenoxy group, pharmaceutically acceptable methanesulfonate, fumarate, bromate, citrate, maleate, phosphate, sulfate, sodium salt, hydrochlorate or amine not being salt.

Abstract translation: 目的：提供式（I）表示的异恶唑羰基恶唑烷酮衍生物，对革兰氏阳性菌株具有优异的抗菌活性。 此外，提供了该化合物的制备方法。 构成：由式（I）表示的异恶唑基羰基恶唑烷酮衍生物通过在碱和溶剂的存在下酰化通式（II）的恶唑烷酮衍生物和通式（III）的羧酸衍生物来制备。 式（II）和（III）中的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， 一个氮原子，噻唑，噻二唑，氨基噻唑，异噻唑，异恶唑，恶唑，恶二唑，四唑，吡啶，烷基，卤素，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，药学上可接受的甲磺酸酯， 富马酸盐，溴酸盐，柠檬酸盐，马来酸盐，磷酸盐，硫酸盐，钠盐，盐酸盐或胺不是盐。

公开(公告)号：KR100234014B1

公开(公告)日：1999-12-15

申请号：KR1019970053271

申请日：1997-10-17

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  고훈영 ,  배애님 ,  김명주 ,  차주환 ,  장문호 ,  최경일 ,  하영진

IPC: C07D499/08

Abstract: 본 발명은 일반식( II )의 알데히드와 일반식( III )의 할로겐염 유도체를 이중결합시켜 중간체인 일반식( IV )의 비닐 화합물을 제조하고 카르복시 보호기를 제거하여 일반식(I)로 표시되는 신규한 2-베타-알케닐-페남 유도체를 제조하며, 이는 베타락타마제 저해제로서 기존의 항생제와 일정 비율로 병용하면 항균작용을 증진시키는 유용한 화합물이다.