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公开(公告)号：KR1019900003562B1
公开(公告)日：1990-05-21
申请号：KR1019870014208
申请日：1987-12-22
Applicant: 한국과학기술연구원
IPC: C07D501/20 , C07D501/22 , C07D501/34
Abstract: Silly cephalosporin derivs. having formula (I) are new. (I) are prepd. by reacting sillyl cpds. with cephalosporin in the presence of org. solvent (i.e. acetone, dioxane, THF) and acid (i.e. formic acid, acetic acid, propionic acid) or base (i.e. alkali metal hydroxide, N,N-di (lower)-alkylbenzyl amine) at 0-25 deg. C. In (I), R=H or trithyl; R2= acetoxymethyl or vinyl; R3= H or Na; n= 1; X= Y= Z=Me. (I) show broad spectrum against gram positive and gram negative.
Abstract translation: 愚蠢头孢菌素衍生物。 具有式（I）的化合物是新的。 （I）是prepd。 通过使硅烷基cpds反应。 头孢菌素在组织的存在下。 溶剂（即丙酮，二恶烷，THF）和酸（即甲酸，乙酸，丙酸）或碱（即碱金属氢氧化物，N，N-二（低级 - 烷基苄基胺））在0-25℃。 C.（I）中，R = H或三硫代基; R2 =乙酰氧基甲基或乙烯基; R3 = H或Na; n = 1; X = Y = Z = Me。 （I）显示广谱对革兰氏阳性和革兰氏阴性。
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公开(公告)号：KR1019900003407B1
公开(公告)日：1990-05-18
申请号：KR1019870014207
申请日：1987-12-12
Applicant: 한국과학기술연구원
IPC: C07D277/28 , C07F7/10
Abstract: A silyl cpd. of formula (I) is prepd. by reacting an ester cpd. of formula (II) with a halosilan cpd. of formula M-(CH2)n- Si (X)(Y)(Z) in the presence of solvent i.e. DMF, MeOH and base i.e. NaOH, Na2CO3 at 10-30 deg. C. In the formulas, R1=H or trityl gp.; R2= carboxy or methylester gp.; M=I; X= Y= Z= Me; n=1. (I) is useful as an intermediate for the prodn. of cephalosporin cpds.
Abstract translation: 甲硅烷基cpd 式（I）的化合物是制备的。 通过使酯cpd反应。 的式（II）与卤代硅烷cpd。 在溶剂存在下，即DMF，MeOH和碱，即NaOH，Na 2 CO 3，在10-30℃，式M-（CH 2）n -Si（X）（Y）（Z） 式中，R 1 = H或三苯甲基。 R2 =羧基或甲酯gp。 M = I; X = Y = Z = Me n = 1时。 （I）可用作产品的中间体。 的头孢菌素cpds。
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公开(公告)号：KR1019890009940A
公开(公告)日：1989-08-05
申请号：KR1019870014208
申请日：1987-12-22
Applicant: 한국과학기술연구원
IPC: C07D501/20 , C07D501/22 , C07D501/34
Abstract: 내용 없음
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Patent Agency Ranking
公开(公告)号：KR100716103B1
公开(公告)日：2007-05-09
申请号：KR1020050102341
申请日：2005-10-28
Applicant: 한국과학기술연구원
Abstract: 본 발명은 신경 세포내 T-형 칼슘 채널 (T-type calcium channel) 차단제 개발에 유용하고 그 개발기간을 단축시키는, 형광 이미징 HTS 측정법을 이용한 α1G T-형 또는 α1H T-형 칼슘 채널 차단제의 고효율 검색 방법 (High-throughput screening, HTS)에 관한 것이다. T-형 칼슘 채널 차단제는 세포막의 칼슘 채널을 억제하여 협심증, 고혈압, 심근질환, 통증, 간질과 같은 다수의 질환을 치료 및 예방하는데 유용하다.
T-형 칼슘 채널, 형광 칼슘이미징 측정법, 심근질환, 간질, 통증, 패치클램프Abstract translation: 使用荧光成像测定以HTS高效型或α1Hα1GT- T-型钙通道阻滞剂的发明是有用的缩短开发时间T-型钙离子通道（T型钙通道）神经元阻断剂内发展 和高通量筛选（HTS）。 T型钙通道阻滞剂抑制细胞膜中的钙通道，可用于治疗和预防许多疾病，如心绞痛，高血压，心肌疾病，疼痛和癫痫。
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公开(公告)号：KR100645371B1
公开(公告)日：2006-11-14
申请号：KR1020050061697
申请日：2005-07-08
Applicant: 한국과학기술연구원
IPC: C07D493/04
Abstract: Novel bicyclic tetrahydrofuran derivatives, and a process for preparing the same compounds are provided to improve efficiency of preparation, so that they are useful as intermediates for synthesis of natural products. The bicyclic tetrahydrofuran derivatives represented by the formula(1) are provided, wherein n is 1 or 2; R is phenyl group or substituted phenyl group by C1-C6 alkyl group, C1-C6 alkoxy group, hydroxy group or C1-C6 hydroxyalkyl group; and R1 is C1-C6 alkyl group. The bicyclic tetrahydrofuran derivatives represented by the formula(1) are prepared by intramolecular cyclizing tetrahydrofuran-allenol derivatives in the presence of alcohol compounds, transition metal catalyst and carbon monoxide(CO), wherein the transition metal catalyst is palladium chloride or copper chloride; and the reaction temperature is 0 to 25 deg.C.
Abstract translation: 新型双环四氢呋喃衍生物及其制备方法可提高制备效率，因此它们可用作合成天然产物的中间体。 提供由式（1）表示的双环四氢呋喃衍生物，其中n是1或2; R 1为C 1 -C 6烷基，C 1 -C 6烷氧基，羟基或C 1 -C 6羟烷基的苯基或取代的苯基; 并且R 1是C 1 -C 6烷基。 由式（1）表示的双环四氢呋喃衍生物是在醇化合物，过渡金属催化剂和一氧化碳（CO）存在下通过分子内环化四氢呋喃 - 烯醇衍生物制备的，其中过渡金属催化剂为氯化钯或氯化铜; 反应温度为0〜25℃。
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公开(公告)号：KR1020060026315A
公开(公告)日：2006-03-23
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：KR100488444B1
公开(公告)日：2005-05-11
申请号：KR1020010089274
申请日：2001-12-31
Applicant: 한국과학기술연구원
IPC: C07D215/56
Abstract: 다음 화학식 6의 헤테로고리 화합물 및 그의 제조 방법;
화학식 6
식 중에서, R은 H이거나 Cl, F, Br 및 I에서 선택되는 할로겐 원소이고; R
1 와 R
2 는 서로 독립적으로 H, 알킬기 또는 -OH기이며, Y는 -Ts(토실), -Ms(메실) 또는 -Ac(아세틸)임.-
公开(公告)号：KR1020050028095A
公开(公告)日：2005-03-22
申请号：KR1020030064384
申请日：2003-09-17
Applicant: 한국과학기술연구원
IPC: C07D493/08
CPC classification number: C07D493/08 , A61K31/343
Abstract: A 8-membered cyclic compound having diexomethylene groups and a preparation method thereof are provided, which compound is useful as an intermediate for preparing other cyclic compound through Diels-Alder reaction, and has improved activity. The 8-membered cyclic compound having diexomethylene groups represented by formula (1) is provided, wherein R1 is phenyl; R2 and R3 are independently hydrogen; or R1, R2 and R3 together form 5- to 10-membered aliphatic or aromatic rings. The method for preparing the 8-membered cyclic compound having diexomethylene groups represented by formula (1) comprises cyclization of trimethylsilanylmethyl-alenol derivatives in the presence of Lewis acid in solvent at -90 deg. C to the room temperature, wherein the solvent is selected from diethylether, tetrahydrofuran, dichloromethane and chloroform; and the Lewis acid is trimethylsillyl trifluoromethanesulfonate(TMSOTf).
Abstract translation: 提供具有阴离子亚甲基的8元环状化合物及其制备方法，该化合物可用作通过Diels-Alder反应制备其它环状化合物的中间体，并且具有改善的活性。 提供了由式（1）表示的具有正亚烷基的8元环状化合物，其中R 1是苯基; R2和R3独立地是氢; 或R 1，R 2和R 3一起形成5至10元脂族或芳环。 由式（1）表示的具有阴离子亚甲基的8-元环状化合物的制备方法包括在路易斯酸存在下，在-90℃的溶剂中使三甲基硅烷基甲基 - 烯醇衍生物环化。 C至室温，其中溶剂选自乙醚，四氢呋喃，二氯甲烷和氯仿; 路易斯酸是三甲基甲硅烷基三氟甲磺酸酯（TMSOTf）。
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