公开(公告)号：KR1020040001435A

公开(公告)日：2004-01-07

申请号：KR1020020036636

申请日：2002-06-28

Applicant: 한국화학연구원

Inventor： 김문환 ,  심영기 ,  이광재 ,  이수헌 ,  류의상 ,  안승호

IPC: C07C231/12

Abstract: PURPOSE: Provided is a method for preparing an atorvastatin synthetic intermediate, 4-(4-fluorophenyl)-2-isobutyryl-3-phenyl-4-oxo-N-phenylbutyramide under a mild condition in a short time by a simple process at a high yield and with a high purity. CONSTITUTION: The method for preparing 4-(4-fluorophenyl)-2-isobutyryl-3-phenyl- 4-oxo-N-phenylbutyramide represented by the formula 2 comprises the step for carrying out the nucleophilic substitution reaction of 4-methyl-3-oxo-N-phenylpentamide represented by the formula 3 with 2-halo-1-(4-fluorophenyl)2-phenone represented by the formula 4 or 2,2-dihalo-1- (4-fluorophenyl)-2-phenone represented by the formula 5, or the mixture thereof in the presence of a base, wherein X is Cl, Br or I.

Abstract translation: 目的：提供一种在短时间内通过简单方法在温和条件下制备阿托伐他汀合成中间体4-（4-氟苯基）-2-异丁酰基-3-苯基-4-氧代-N-苯基丁酰胺的方法， 高产量和高纯度。 构成：由式2表示的4-（4-氟苯基）-2-异丁酰基-3-苯基-4-氧代-N-苯基丁酰胺的制备方法包括进行4-甲基-3的亲核取代反应的步骤 由式3代表的2-卤代-1-（4-氟苯基）-2-苯酮或2,2-二卤代-1-（4-氟苯基）-2-苯酮代表的由式3表示的2-氧代-N-苯基戊酰胺代表 通式5，或其在碱存在下的混合物，其中X为Cl，Br或I.

公开(公告)号：KR100128513B1

公开(公告)日：1998-04-04

申请号：KR1019940012482

申请日：1994-06-03

Applicant: 한국화학연구원

Inventor： 김완주 ,  김경수 ,  정희정 ,  심영기 ,  나차수 ,  황태섭 ,  이미정 ,  안구현 ,  김홍기

IPC: C07D499/88 ,  C07D499/86

Abstract: (5R,6S)-6((1R)-1-hydroxyethyl)-2-((5R)-5-oxazolidinonyl)-3-carboxyl-2-penem derivatives(I; R= H atom, methyl, ethyl, phenyl, aryl ring compound substituted by oxygen, nitrogen or sulphur; R1= H or ester forming group hydrolyzed in a biomass, indanyl, phthalidyl, methoxymethyl, glycycloxymethyl, phenylglycycloxymethyl, etc.) were prepared. Thus, 250 mg (5R)-5-carboxyl-3-t-butyldiphenylsilyl oxazolidinone was dissolved at 0 deg.C in 150 ml dichloromethane, and added 27.1 ml 60 % sodium hydride, 0.06 ml pyridin at -30 deg.C, 0.05 ml thionyl chloride, reacted at room temperature for 2 hours. 0.56 g (3S,4R)-3-(1-(R)-t-butyldimethylsilyloxyethyl)-1-(1-(4-nitrobenzyloxy-carbonyl)-1-(triphenylphosphoranylidene)methyl)azetidin-2-one-4-thiolate was reacted with the reactant to give 430 mg (3S,4R)-3-(1-(R)-t- butyldimethylsilyloxyethyl)-4-((5R)-5-(3-t-butyldiphenylsilyloxazolidinonyl)carbothio)-1-(1-(4-nitrobenzyloxycarbonyl)-1-(triphenylphosphoranylidene)methyl)azetidinone.

Abstract translation: （5R，6S）-6（（1R）-1-羟乙基）-2 - （（5R）-5-恶唑烷酮基）-3-羧基-2-季戊四醇衍生物（I; R = H原子，甲基，乙基， 被氧，氮或硫取代的芳环化合物; R1 = H或在生物质中水解的酯形成基团，茚满基，苯并吡喃基，甲氧基甲基，乙酰氧基甲基，苯基乙酰氧基甲基等）。 因此，将250mg（5R）-5-羧基-3-叔丁基二苯基甲硅烷基恶唑烷酮在0℃下在150ml二氯甲烷中溶解，并在-30℃下加入26.1ml 60％氢化钠，0.06ml吡啶，0.05 的亚硫酰氯，在室温下反应2小时。 0.56g（3S，4R）-3-（1-（R） - 叔丁基二甲基甲硅烷氧基乙基）-1-（1-（4-硝基苄氧羰基）-1-（三苯基亚正膦基）甲基）氮杂环丁烷-2-酮-4- 将硫醇盐与反应物反应，得到430mg（3S，4R）-3-（1-（R） - 叔丁基二甲基甲硅烷氧基乙基）-4 - （（5R）-5-（3-叔丁基二苯基甲硅烷氧基唑烷基）碳硫基） - （1-（4-硝基苄氧羰基）-1-（三苯基膦烯）甲基）氮杂环丁酮。

公开(公告)号：KR1019960000892A

公开(公告)日：1996-01-25

申请号：KR1019940012482

申请日：1994-06-03

Applicant: 한국화학연구원

Inventor： 김완주 ,  김경수 ,  정희정 ,  심영기 ,  나차수 ,  황태섭 ,  이미정 ,  안구현 ,  김홍기

IPC: C07D499/88 ,  C07D499/86

Abstract: 본 발명은 합성β-락탐계의 신규한 페넴 화합물의 유도체 및 그의 제조방법으로, 특히 트란스 형태의 2-치환-2-페넴-3-카복실산 화합물에 관한 것이다.
즉, 본 발명은 다음구조식(I)의 (5R,6S)-6-[(1R)-1-히드록시에틸]-2-[(5R)-5-옥사졸리디노닐]-3-카복실-2-페넴 유도체와 식(Ⅱ)의 (5R,6S)-6-[(1R)-1-히드록시에틸]-2-[((5R)-5-옥사졸리디노닐)메틸티오]-3-카복실-2-페넴 유도체 및 그들의 제조방법이다.

윗 식에서, R은 수소원자, 메틸, 에틸, 페닐, 아릴, 산소 질소 또는 황으로 치환된 고리 화합물이며, R
1 은 수소이거나 또는 생체내에서 가수분해되는 에스테르를 형성하는 군을 포함한다.

公开(公告)号：KR100039539B1

公开(公告)日：1991-02-02

申请号：KR1019880016744

申请日：1988-12-15

Applicant: 한국화학연구원

Inventor： 김완주 ,  심영기 ,  전재상

IPC: C07D211/82

公开(公告)号：KR1019900007623B1

公开(公告)日：1990-10-17

申请号：KR1019880016744

申请日：1988-12-15

Applicant: 한국화학연구원

Inventor： 김완주 ,  심영기 ,  전재상

IPC: C07D211/82

Abstract: 1,4-Dihydropyridine derivs. of formula (I) are prepared. In (I), R1 and R2 are each C1-6 alkyl, lower alkenyl, lower alkoxyalkyl or aminoaryl (lower)alkyl opt. substd. by C1-4 alkyl; at least one of R1 and R2 is C3-6 alkenyl opt. substd. by C1-4 alkyl at 1- or 2- position; R3 is ortho-, meta- or para-nitro gp. (I) are useful as hypotensives.

Abstract translation: 1,4-二氢吡啶衍生物。 制备式（I）化合物。 在（I）中，R 1和R 2各自为C 1-6烷基，低级烯基，低级烷氧基烷基或氨基芳基（低级）烷基选择。 substd。 通过C 1-4烷基; R 1和R 2中的至少一个是C 3-6烯基选择。 substd。 由1-或2-位上的C 1-4烷基取代; R3是邻 - ，间 - 或对 - 硝基gp。 （I）作为假设是有用的。

公开(公告)号：KR1019900009587A

公开(公告)日：1990-07-04

申请号：KR1019880016744

申请日：1988-12-15

Applicant: 한국화학연구원

Inventor： 김완주 ,  심영기 ,  전재상

IPC: C07D211/82

公开(公告)号：KR1019890002179A

公开(公告)日：1989-04-08

申请号：KR1019870006785

申请日：1987-07-01

Applicant: 한국화학연구원

Inventor： 김완주 ,  김홍범 ,  고광윤 ,  심영기 ,  오중훈

IPC: C07D501/24

Abstract: 내용없음