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公开(公告)号：KR1020000067451A
公开(公告)日：2000-11-15
申请号：KR1019990015261
申请日：1999-04-28
Applicant: 한국과학기술연구원
IPC: C07D501/22
CPC classification number: Y02P20/55
Abstract: PURPOSE: Cepham derivatives prepared by the reaction of 3-hydroxy cephem derivatives and allylhalide or acetylene halide in a solvent in the presence of a metal catalyst and process for the preparation method thereof are provided which can be used as an intermediate for the manufacture of cephem antibiotics. CONSTITUTION: Cepham derivatives of formula (I) useful as an intermediate for producing cephem antibiotics are prepared by the reaction of 3-hydroxy cephem derivatives of formula (V) and allylhalide (III) or acetylene halide in a solvent in the presence of a metal catalyst at 0 to 100°C for 1 to 96 hr. In formula, R1 represents phenylacetyl, 2-£2-amino(1,3-thiazole-4-yl)-2-(hydroxyalkoxyimino)ethinyl, 2-£2-amino(1,3-thiazole-4-yl)-2-(alkoxyimino)ethinyl or 4-hydroxyphenylglycine derivative, R2 is H, carboxylic acid salts (sodium and potassium salt as inorganic salts, alkylamine salt, aromatic amine salt as organic salts), a molecular protecting group in the cephalosporin field of 4-methoxybenzyl, diphenylbenzyl, diphenylmethyl, 4-nitrobenzyl, allyl as a carboxyl protecting group, in a Q compound, R3, R4 and R5 represent each H, halogen, methyl, ethyl, hydroxy, phenyl or alkoxycarbonyl.
Abstract translation: 目的：提供在金属催化剂存在下，通过3-羟基头孢烯衍生物和烯丙基卤或乙炔卤化物在溶剂中反应制备的Cepham衍生物，其制备方法可用作中间体，用于制备头孢烯 抗生素。 构成：通过式（Ⅴ）的3-羟基头孢烯衍生物与烯丙基卤（III）或炔酰卤在溶剂中在金属存在下的反应制备用作产生头孢类抗生素的中间体的式（I）的头孢类衍生物 催化剂在0〜100℃下反应1〜96小时。 在式中，R 1表示苯乙酰基，2- {2-氨基（1,3-噻唑-4-基）-2-（羟基烷氧基亚氨基）乙炔基，2-（2-氨基（1,3-噻唑-4-基） 2-（烷氧基亚氨基）乙炔基或4-羟基苯基甘氨酸衍生物，R2是H，羧酸盐（作为无机盐的钠盐和钾盐，烷基胺盐，作为有机盐的芳族胺盐），四氢呋喃的头孢菌素领域中的分子保护基， 甲氧基苄基，二苯基苄基，二苯基甲基，4-硝基苄基，烯丙基作为羧基保护基，在Q化合物中，R 3，R 4和R 5各自表示H，卤素，甲基，乙基，羟基，苯基或烷氧基羰基。
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公开(公告)号：KR100267260B1
公开(公告)日：2000-11-01
申请号：KR1019980027115
申请日：1998-07-06
Applicant: 한국과학기술연구원
IPC: C07D501/24 , C07D501/20
Abstract: 본 발명은 경구 투여가 가능한 새로운 세펨 에스테르 화합물 및 이의 제조방법에 관한 것으로, 그램 양성균과 그램 음성균에 대해 광범위의 항균력을 나타내며, 특히 MRSA를 포함한 여러 내성균에 강한 항균력을 나타내는 약제학적으로 유용한 화합물이다.
(I)
일반식 (I)에 있어서, R
1 은 수소 또는 트리틸기를 표시하며, R
2 는 수소, 트리틸기, 메틸기 또는 시클로펜틸기를 표시하며, R
3 는 수소, 클로로, 브로모 또는 메톡시기를 표시하며, R
4 는 아세톡시에틸, 피발로일옥시메틸 또는 이소프로폭시카르보닐옥시에틸기를 표시한다.-
公开(公告)号：KR1020000002400A
公开(公告)日：2000-01-15
申请号：KR1019980023118
申请日：1998-06-19
Applicant: 한국과학기술연구원
IPC: C07D453/00 , C07D261/20
Abstract: PURPOSE: The compound is provided which exhibits a high affinity for muscarinic acetylcholine receptor and is useful as therapeutic agent of cerebral nerve disease such as Alzheimer's disease. CONSTITUTION: The carbonyl compound of the formula (II), wherein, n is integer 1 or 2, is reacted with phosphonium salt compound of formula (III), in which R is H, halo, alkoxy, cyano, alkyl, alkenyl, alkinyl, hydroxy, amino, nitro, 4-methoxybenzyloxy, t-butoxycarbonylamino or its salt; R1, R2 and R3 are alkyl, aryl or aralkyl, respectively; X is halogen, or with phosphonate compound of the formula (IV) in the presence of solvent and base to give £(aryl) isooxozolyl| methylene-azabicyclo compound of the formula (I). Thus, 188mg of potassium t-butoxide and 482mg of diethyl 3-(4-methylphenyl)-5-isooxazolylmethylphosphonate being dissolved in tetrahydrofuran are stirred for 30 minutes at 22°C to give 3-£3-(4-methylphenyl)isooxazol-5-yl|methylene-1-azabicyclo£2.2.2|octane oxalic acid salt.
Abstract translation: 目的：提供对毒蕈碱性乙酰胆碱受体具有高亲和力的化合物，并且可用作脑神经疾病如阿尔茨海默病的治疗剂。 构成：其中n为1或2的式（II）的羰基化合物与式（III）的鏻盐化合物反应，其中R为H，卤素，烷氧基，氰基，烷基，烯基，炔基 ，羟基，氨基，硝基，4-甲氧基苄氧基，叔丁氧基羰基氨基或其盐; R1，R2和R3分别是烷基，芳基或芳烷基; X为卤素，或与式（IV）的膦酸酯化合物在溶剂和碱存在下反应，得到（芳基）异恶唑基| 式（I）的亚甲基 - 氮杂二环化合物。 因此，将188mg叔丁醇钾和482mg 3-（4-甲基苯基）-5-异恶唑甲基膦酸二乙酯溶于四氢呋喃中，在22℃下搅拌30分钟，得到3- {3-（4-甲基苯基）异恶唑-4-基） 5-基|亚甲基-1-氮杂双环{2.2.2 |辛酸草酸盐。
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公开(公告)号：KR100645373B1
公开(公告)日：2006-11-14
申请号：KR1020050061721
申请日：2005-07-08
Applicant: 한국과학기술연구원
IPC: C07D493/04
Abstract: Novel tricyclic tetrahydrofuran lactone derivatives, and a preparation process thereof are provided to reduce the preparation procedures of tricyclic tetrahydrofuran lactone derivatives into one step, so that preparation costs are reduced. The tricyclic tetrahydrofuran lactone derivatives represented by the formula(1) are provided in which R is phenyl group optionally substituted by C1-C6 alkyl group, C1-C6 alkoxy group, hydroxy group or C1-C6 hydroxyalkyl group; and R1 is hydrogen, C1-C6 alkyl group, C1-C6 alkoxy group, hydroxy group or C1-C6 hydroxyalkyl group. The tricyclic tetrahydrofuran lactone derivatives represented by the formula(1) are prepared by intramolecular cyclizing tetrahydrofuran-allenic acid derivatives represented by the formula(2) in the presence of phenyl halide, palladium catalyst and base; the reaction solvent is diethylether, tetrahydrofuran, dichloromethane, dimethylformamide, ethylacetate or chloroform; the palladium catalyst is tetrakis(triphenylphosphin) palladium; the base is carbonate, hydrogen carbonate or sulfate of alkali metals or alkali earth metals; and the reaction temperature is 0 to 90 deg.C.
Abstract translation: 提供新型三环四氢呋喃内酯衍生物及其制备方法，以将三环四氢呋喃内酯衍生物的制备过程减少为一步，从而降低制备成本。 提供了式（1）所示的三环四氢呋喃内酯衍生物，其中R为任选被C1-C6烷基，C1-C6烷氧基，羟基或C1-C6羟烷基取代的苯基; 和R1是氢，C1-C6烷基，C1-C6烷氧基，羟基或C1-C6羟烷基。 由式（1）表示的三环四氢呋喃内酯衍生物是在苯基卤化物，钯催化剂和碱的存在下，通过分子内环化式（2）表示的四氢呋喃 - 反应溶剂是乙醚，四氢呋喃，二氯甲烷，二甲基甲酰胺，乙酸乙酯或氯仿; 钯催化剂是四（三苯基膦）钯; 碱是碱金属或碱土金属的碳酸盐，碳酸氢盐或硫酸盐; 反应温度为0〜90℃。
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Patent Agency Ranking
公开(公告)号：KR100545785B1
公开(公告)日：2006-01-24
申请号：KR1020030055099
申请日：2003-08-08
Applicant: 한국과학기술연구원
IPC: C07D401/06
Abstract: 본 발명은 피페라지닐알킬 트리아졸 화합물에 관한 것으로서, 도파민 수용체에 대한 선택적 길항작용을 가지고 있어 정신병 치료제로 유효한 다음 화학식 1로 표시되는 피페라지닐알킬 트리아졸 화합물과 이 화합물을 용액상 조합 합성법을 이용하여 제조하는 방법, 그리고 이 화합물을 유효성분으로 함유하는 약제조성물에 관한 것이다.
상기 화학식 1에서, n, R
1 , R
2 및 R
3 은 각각 발명의 상세한 설명에서 정의한 바와 같다.
피페라지닐알킬 트리아졸, 도파민 수용체, 정신병 치료제Abstract translation: 本发明的血液约烷基三唑类化合物，哌嗪烷基三唑化合物和由下式表示的化合物的哌嗪基（1）有效地作为抗精神病药物得到了多巴胺受体具有选择性拮抗溶液相组合的合成 以及含有该化合物作为有效成分的药物组合物。
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公开(公告)号：KR100490643B1
公开(公告)日：2005-05-19
申请号：KR1020020066268
申请日：2002-10-29
Applicant: 한국과학기술연구원
IPC: C07D413/10
CPC classification number: C07D413/10 , C07D413/14 , C07D417/14
Abstract: 본 발명은 아래의 화학식 1로 표시되는 메틸리덴 피페리딘일 옥사졸리딘온 유도체 화합물, 그 염 및 이들의 제조방법에 관한 것이다. 본 발명의 화합물은 메티실린 저항성 스타필로코코스 아우레우스 및 반코마이신 저항성 엔테로코코스 등과 같은 내성 균주를 포함하는 그람 양성균에 대하여 우수한 항균 활성을 나타낸다.
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公开(公告)号：KR1020050017158A
公开(公告)日：2005-02-22
申请号：KR1020030055099
申请日：2003-08-08
Applicant: 한국과학기술연구원
IPC: C07D401/06
Abstract: PURPOSE: Piperazinyl alkyl triazole compounds having selectively inhibiting activity at dopamine receptors are provided, which compounds are dopamine antagonists, so that they can be useful for treatment of psychomancy disease. CONSTITUTION: The piperazinyl alkyl triazole compounds represented by formula (1) or pharmaceutically acceptable salts thereof are provided, wherein n is an integer of 3 or 4; R1 is optionally substituted phenyl or optionally substituted benzhydryl, in which the substituent is C1-C6 alkyl, C1-C6 alkoxy, hydroxy, C1-C6 hydroxyalkyl, aryl, heteroaryl, amino, C1-C6 alkylamino, C2-C6 alkenyl, carbonyl, C3-C9 cycloalkyl and C3-C9 hetero ring; and R2 and R3 are independently hydrogen, C1-C6 alkyl or C1-C6 alkylester. A method for preparing the piperazinyl alkyl triazole compounds of formula (1) comprises reacting azide compound of formula (2) with alkylester compound of formula (3) in solution through combinatorial synthesis, wherein the solvent is dimethylformamide or acetonitrile.
Abstract translation: 目的：提供在多巴胺受体上具有选择性抑制活性的哌嗪基烷基三唑化合物，这些化合物是多巴胺拮抗剂，因此它们可用于治疗心理病。 构成：提供由式（1）表示的哌嗪基烷基三唑化合物或其药学上可接受的盐，其中n为3或4的整数; R1是任选取代的苯基或任选取代的二苯甲基，其中取代基是C1-C6烷基，C1-C6烷氧基，羟基，C1-C6羟基烷基，芳基，杂芳基，氨基，C1-C6烷基氨基，C2-C6烯基，羰基， C3-C9环烷基和C3-C9杂环; 且R 2和R 3独立地是氢，C 1 -C 6烷基或C 1 -C 6烷基酯。 制备式（1）的哌嗪基烷基三唑化合物的方法包括通过组合合成使式（2）的叠氮化合物与式（3）的烷基酯化合物在溶液中反应，其中溶剂是二甲基甲酰胺或乙腈。
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公开(公告)号：KR100380324B1
公开(公告)日：2003-04-16
申请号：KR1020000009065
申请日：2000-02-24
Applicant: 한국과학기술연구원
IPC: C07D501/16
CPC classification number: Y02P20/55
Abstract: PURPOSE: Provided is a cephem derivative which has broad range of antimicrobial activity. And its producing method is also provided. CONSTITUTION: The cephalosporin compounds represented by formula (1) and its pharmaceutically acceptable salts are produced. In the formula, R1 is hydrogen or an amine protecting group generally used in cephalosporin compounds; R2 is hydrogen or an oxim protecting group; R3 is hydrogen or a chloro group; R5 is hydrogen or an ester producing group, a salt producing atom or a carboxy protecting group; and R4 is ring substituent having Q group, in which Q is hydrogen, halogen, hydroxy, mercapto, cyano, carboxy, carboxylic acid ester, carbamoyloxymethyl, N,N-dimethylcarbamoyloxymethyl, carbamoyl, N,N-dimethylcarbamoyl, C1 to C4 alkyl, C1 to C4 alkyloxy, halogen substituted methyl, halogen substituted C1 to C4 alkyloxy, aryl or hetero ring substituent. The cephalosporin derivative of formula (1) is produced by reacting a compound of formula (7) with a compound of formula (8).
Abstract translation: 目的：提供具有广泛抗微生物活性的头孢烯衍生物。 并提供其制作方法。 构成：生产式（1）代表的头孢菌素化合物及其药学上可接受的盐。 在该式中，R1是氢或通常用于头孢菌素化合物中的胺保护基; R2是氢或肟保护基; R3是氢或氯基; R5是氢或产酯基团，产盐原子或羧基保护基团; 其中Q为氢，卤素，羟基，巯基，氰基，羧基，羧酸酯，氨基甲酰氧基甲基，N，N-二甲基氨基甲酰氧基甲基，氨基甲酰基，N，N-二甲基氨基甲酰基，C1-C4烷基， C1至C4烷氧基，卤素取代的甲基，卤素取代的C1至C4烷氧基，芳基或杂环取代基。 式（1）的头孢菌素衍生物通过使式（7）的化合物与式（8）的化合物反应来制备。
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公开(公告)号：KR100380322B1
公开(公告)日：2003-04-16
申请号：KR1020000009063
申请日：2000-02-24
Applicant: 한국과학기술연구원
IPC: C07D501/16
CPC classification number: Y02P20/55
Abstract: PURPOSE: Provided is an isothiazol cephem derivative which has broad range of antimicrobial activity. And its producing method is also provided. CONSTITUTION: The cephalosporin compound represented by formula (1) and its pharmaceutically acceptable salts are produced. In the formula, R1 is hydrogen or an amine protecting group generally used in cephalosporin compound; R2 is hydrogen or an oxim protecting group; R3 is hydrogen or a chloro group; R5 is hydrogen or an ester producing group, a salt producing atom or a carboxy protecting group; and R4 is ring substituent having Q group, in which Q is hydrogen, halogen, hydroxy, mercapto, cyano, carboxy, carboxylic acid ester, carbamoyloxymethyl, N,N-dimethylcarbamoyloxymethyl, carbamoyl, N,N-dimethylcarbamoyl, C1 to C4 alkyl, C1 to C4 alkyloxy, halogen substituted methyl, halogen substituted C1 to C4 alkyloxy, aryl or hetero ring substituent. The cephalosporin derivative of the formula (1) is produced by reacting a compound of formula (7) with a compound of formula (8).
Abstract translation: 目的：提供具有广泛抗微生物活性的异噻唑头孢烯衍生物。 并提供其制作方法。 构成：由式（1）表示的头孢菌素化合物及其药学上可接受的盐被制备。 在该式中，R1是氢或通常用于头孢菌素化合物中的胺保护基; R2是氢或肟保护基; R3是氢或氯基; R5是氢或产酯基团，产盐原子或羧基保护基团; 其中Q为氢，卤素，羟基，巯基，氰基，羧基，羧酸酯，氨基甲酰氧基甲基，N，N-二甲基氨基甲酰氧基甲基，氨基甲酰基，N，N-二甲基氨基甲酰基，C1-C4烷基， C1至C4烷氧基，卤素取代的甲基，卤素取代的C1至C4烷氧基，芳基或杂环取代基。 式（1）的头孢菌素衍生物通过使式（7）的化合物与式（8）的化合物反应来制备。
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