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公开(公告)号：KR100623272B1
公开(公告)日：2006-09-12
申请号：KR1020050061730
申请日：2005-07-08
Applicant: 한국과학기술연구원
IPC: C07D307/93
Abstract: 본 발명은 세 고리형 테트라하이드로퓨란 화합물과 이의 제조방법에 관한 것으로서, 더욱 상세하게는 테트라하이드로퓨란-알렌 유도체를 출발물질로 사용하여 금속 촉매와 소듐 아자이드(NaN
3 )가 존재하는 조건하에서 분자내 고리화 반응을 통해 제조되어지는, 다음 화학식 1로 표시되는 신규 구조의 물질로서 세 고리형 테트라하이드로퓨란 화합물과 이의 제조방법에 관한 것이다.
상기 화학식 1에서, n은 0 또는 1의 정수를 나타내며; R은 페닐기 또는 치환된 페닐기를 나타내고, 이때 치환체는 C
1 -C
6 의 알킬기, C
1 -C
6 의 알콕시기, 하이드록시기, 및 C
1 -C
6 의 하이드록시알킬기 중에서 선택되고; R
1 은 수소원자, 할로겐원자, C
1 -C
6 의 알킬기, C
1 -C
6 의 알콕시기, 하이드록시기, 및 C
1 -C
6 의 하이드록시알킬기 중에서 선택된다.
세 고리 테트라히드로퓨란 화합물, 분자내 고리화 반응, 알렌Abstract translation: 本发明涉及一种三个环形四氢呋喃化合物及其制备方法，并且更特别是四氢呋喃-使用Allen衍生物作为起始原料的金属催化剂和叠氮化钠（NaN的
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公开(公告)号：KR100616099B1
公开(公告)日：2006-08-28
申请号：KR1020040075192
申请日：2004-09-20
Applicant: 한국과학기술연구원
IPC: C07D413/14 , C07D413/12
Abstract: 본 발명은 T-타입 칼슘채널(T-type calcium channel)에 대한 선택적인 길항작용이 우수하여 이와 관련된 뇌질환 및 심장질환의 치료 및 예방에 유효한 피페라지닐알킬 이소옥사졸 유도체와 용액상 조합 합성을 이용한 이 화합물의 제조방법 그리고 이 화합물의 T-타입 칼슘 길항제로서의 의약적 용도에 관한 것이다.
피페라지닐알킬 이소옥사졸, T-타입 칼슘채널, 간질, 고혈압-
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
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。
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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
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。
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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
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。
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Patent Agency Ranking
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
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。
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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
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。
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公开(公告)号：KR1019950008318B1
公开(公告)日：1995-07-27
申请号：KR1019920012641
申请日：1992-07-15
Applicant: 한국과학기술연구원
IPC: C07D501/20
CPC classification number: Y02A50/473 , Y02A50/481
Abstract: This is new cephalosphorin compd. and its parmaceutically acceptable salt of formula(I). In formula, R1 is H, or trityl, tert-butoxycarbonyl, or formyl; R2 hydrogen, p-methoxybenzyl, diphenylmethyl, or salting compd. such as Na or K; R3 and R4 are same or different, and H, p-methoxybenzyl or diphenylmethyl; and Q hydrogen, chloro, vinyl, acetoxymethyl, halomethyl, N- ethylpyridiniumylthiomethyl, N- carboxymethyl pyridiniumyl thiomethyl, and N- methyl- tetrazolyl thiomethyl gp. This cephem compd. manufacturing method comprises A) condensing the amine compd. of (VIII) with ketone of (VII) and producing the compd of (II); and B) acylating the aminothiazol compd of (II) with cephalosphorin of (III). This cephem compd. has good antibacterial activity.
Abstract translation: 这是新头孢菌素 和其药学上可接受的式（I）盐。 在式中，R 1是H或三苯甲基，叔丁氧基羰基或甲酰基; R2氢，对甲氧基苄基，二苯基甲基或盐析化合物。 如Na或K; R3和R4相同或不同，H，对甲氧基苄基或二苯基甲基; 和Q氢，氯，乙烯基，乙酰氧基甲基，卤代甲基，N-乙基吡啶鎓硫基甲基，N-羧甲基吡啶鎓硫代甲基和N-甲基 - 四唑基硫代甲基gp。 这个cephem compd 制造方法包括：A）冷凝胺化合物。 （VIII）与（Ⅶ）的酮反应并制备（Ⅱ）化合物; 和B）用（III）的头孢菌素酰化（II）的氨基噻唑化合物。 这个cephem compd 具有良好的抗菌活性。
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公开(公告)号：KR1019930007813B1
公开(公告)日：1993-08-20
申请号：KR1019910018792
申请日：1991-10-25
Applicant: 한국과학기술연구원
IPC: C07D501/24
Abstract: Pyridonium alkenyl cephalosporin derivs. of formula (I) and their pharmaceutical salts are new. 3-Cephem compds. were obtained by witting reaction from a phosphonium cpd. of formula (II) with an aldehyde cpd. of formula (III) and then were deacylated to produce 7-amino-3-cephem derivs. The formula (I) derivs. are prepd. by acylation of 7-amino-3-cephem derivs. with 2- aminothiazolyl- 2-hydroxyimino-acetic acid compds. In (I), R1=H or a protecting gp. as in cephalosporin and penicillin cpds.; R2=H, C1-4 alkyl or substd. alkyl; R3=H or a deriv. of a carboxy gp., an atom for prepn. of a salt or carboxy protecting gp.
Abstract translation: 吡啶鎓烯基头孢菌素衍生物。 的式（I）化合物及其药用盐是新的。 3-Cephem compds 通过从cpd鏻反应得到。 式（II）与醛cpd反应。 的式（III），然后脱酰基以产生7-氨基-3-头孢烯衍生物。 公式（I）导出。 是prepd 通过7-氨基-3-头孢烯衍生物的酰化。 与2-氨基噻唑-2-基亚氨基 - 乙酸组成。 在（I）中，R1 = H或保护gp。 如头孢菌素和青霉素cpds。 R2 = H，C1-4烷基或取代基。 烷基; R3 = H或衍生物。 的羧基，一个原子的制备。 的盐或羧基保护gp。
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