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公开(公告)号：KR1020000073204A
公开(公告)日：2000-12-05
申请号：KR1019990016354
申请日：1999-05-07
Applicant: 한국과학기술연구원
IPC: C07D499/00
CPC classification number: Y02P20/55
Abstract: PURPOSE: A new penam derivative using indium and zinc and a preparation method thereof are provided CONSTITUTION: A novel penam derivative represented by formula(I) is prepared by reacting 6-oxopenam of the formula(I') with ally halide of the formula (II) or acetylene halide of the formula (III) in the presence of indium or zinc. In the formula(I): R1 is allyl derivative and acetylene derivative; R2 is hydrogen, carboxylic acid salt(sodium salt and potassium salt as inorganic salt, alkyl amine salt, aromatic amine salt as organic salt) or carboxy protecting group(4-methoxy benzyl, diphenylmethyl, 4-nitrobenzyl, useful thing as protecting group of molecule in penicillin or cephalosporin compound field); R3 is hydrogen, halogen, hydroxy, acetoxy group.
Abstract translation: 目的：提供使用铟和锌的新的penam衍生物及其制备方法构成：式（I）表示的新型penam衍生物通过式（I'）的6-氧代青霉素与式（I'）的式 II）或式（III）的炔酰卤在铟或锌的存在下进行。 在式（I）中：R 1是烯丙基衍生物和乙炔衍生物; R2为氢，羧酸盐（钠盐和钾盐为无机盐，烷基胺盐，芳族胺盐为有机盐）或羧基保护基（4-甲氧基苄基，二苯基甲基，4-硝基苄基，有用物质为保护基 分子在青霉素或头孢菌素化合物领域）; R3是氢，卤素，羟基，乙酰氧基。
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公开(公告)号：KR1020000051062A
公开(公告)日：2000-08-16
申请号：KR1019990001300
申请日：1999-01-18
Applicant: 한국과학기술연구원
IPC: C07D501/04
Abstract: PURPOSE: A process for preparing 7-aminodesacetoxycephalosporanic acid useful as an important intermediate for preparing cephalosporin antibiotics is provided which comprises reaction of 3-substituted cephalosporin derivatives in the presence of metal indium or an indium compound. CONSTITUTION: A process comprises the steps of preparing a mixture of 7-aminodesacetoxycephalosporanic acid derivatives (I) and 3-exomethylenecephem derivatives (III) by the reaction of 3-substituted cephalosporin derivative (II) in a mixture solution of an organic solvent and water in the presence of solely indium metal or a mixture of indium metal and metal iodide at 10 to 80°C for 1 to 10 hrs and preparing 7-aminodesacetoxycephalosporanic acid (I) by the reaction of the obtained mixture with tetramethylsilylchloride at 20 to 30°C for 20 to 24 hrs.
Abstract translation: 目的：提供一种制备用作制备头孢菌素抗生素的重要中间体的7-氨基脱乙酸基头孢烷酸的方法，其包括在金属铟或铟化合物存在下3-取代头孢菌素衍生物的反应。 构成：一种方法包括通过3-取代头孢菌素衍生物（II）在有机溶剂和水的混合溶液中的反应制备7-氨基脱乙酸基头孢烷酸衍生物（I）和3-异二甲酰头孢烯衍生物（III）的混合物的步骤 在单独的铟金属或铟金属与金属碘化物的混合物的存在下，在10〜80℃下反应1〜10小时，并通过所得混合物与四甲基甲硅烷基氯反应，在20〜30℃下制备7-氨基脱乙酸基头孢烷酸（I） C为20至24小时。
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公开(公告)号：KR1019950008319B1
公开(公告)日：1995-07-27
申请号：KR1019920012642
申请日：1992-07-15
Applicant: 한국과학기술연구원
IPC: C07D501/20
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 H, p-methoxybenzyl, diphenylmethyl or salting compd. such as Na or K; R3 and R4 are same or different, and H, acetyl, or p-methoxybenzyl; X,Y are H, F, Cl, Br, or I; and Q hydrogen, chloro, vinyl, acetoxymethyl, halomethyl, pyridiniummethyl, N- ethyl pyridiniumyl thiomethyl, N- carboxymethyl pyridiniumyl thiomethyl, carbamoyloxymethyl, and N-methyl-tetrazolyl thiomethyl gp. This compd. is prepared by acylation of 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; R2H，对甲氧基苄基，二苯甲基或盐析化合物。 如Na或K; R3和R4相同或不同，H，乙酰基或对甲氧基苄基; X，Y是H，F，Cl，Br或I; 和Q氢，氯，乙烯基，乙酰氧基甲基，卤代甲基，吡啶鎓甲基，N-乙基吡啶鎓硫代甲基，N-羧甲基吡啶鎓硫代甲基，氨基甲酰氧基甲基和N-甲基 - 四唑基硫代甲基gp。 这个compd 通过（II）的氨基噻唑化合物与（III）的头孢菌素的酰化制备。 这个cephem compd 具有良好的抗菌活性。
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公开(公告)号：KR1019930007812B1
公开(公告)日：1993-08-20
申请号：KR1019910018791
申请日：1991-10-25
Applicant: 한국과학기술연구원
IPC: C07D501/24
Abstract: 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: 烯基头孢菌素衍生物。 的式（I）化合物及其药用盐是新的。 3-头孢烯 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-头孢烯衍生物与2-氨基噻唑-2-羟基亚氨基 - 乙酸化合物的酰化反应。 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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公开(公告)号：KR1019930007261B1
公开(公告)日：1993-08-04
申请号：KR1019910006288
申请日：1991-04-19
Applicant: 한국과학기술연구원
IPC: C07D501/24
CPC classification number: C07D257/04 , C07D501/00
Abstract: The cephene-4-carboxylic acid deriv. of formula (I) is prepd. by reacting an aldehyde cpd. of formula (II) with a phosphonium salt of formula (III) in the presence of a base and a solvent at 0-30 deg.C. In the formulas, R1 is methyl, ethyl, propyl, phenyl or benzyl; R2 is p-methoxy benzyl, diphenyl methyl or allyl; R3 is H, t- butoxy carbonyl or phenyl acetyl; R4 is H, t-butoxy carbonyl, formyl or phenyl acetyl. The solvent is pref. water, dichloromethane, ethylether and/or tetrahydrofurane. The deriv. of (I) is useful for antibiotics.
Abstract translation: 环丙烷-4-羧酸衍生物。 式（I）的化合物是制备的。 通过使醛cpd反应。 式（II）的化合物与式（III）的鏻盐在碱和溶剂的存在下在0-30℃下反应。 式中R1是甲基，乙基，丙基，苯基或苄基; R2是对甲氧基苄基，二苯基甲基或烯丙基; R3是H，叔丁氧基羰基或苯基乙酰基; R4是H，叔丁氧基羰基，甲酰基或苯基乙酰基。 溶剂优先。 水，二氯甲烷，乙醚和/或四氢呋喃。 衍生。 （I）可用于抗生素。
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Patent Agency Ranking
公开(公告)号：KR1019930007954A
公开(公告)日：1993-05-20
申请号：KR1019910018791
申请日：1991-10-25
Applicant: 한국과학기술연구원
IPC: C07D501/24
Abstract: 본 발명은 다음 일반식(Ⅰ)로 표시되는 신규한알 케닐세팔로스포린 및 그 제조방법에 관한 것이다.
식 중 R
1 은 수소, 트리틸, 3급 부톡시카르보닐, 포르밀이고, R
2 는 수소, 탄소수 1~4의 알킬, 알콕시카보닐메틸, 카르복시메틸, 1-카르복시에틸, 1-카르복시-1-메틸에틸, 탄소수 3~9의 시클로알킬기이고, R
3 는 수소, 알킬기, Na, K이고, R
4 및 R
5 는 수소 또는 대페닐메틸, 파라메톡시벤질임.
본 발명의 일반식(Ⅰ)로 표시되는 알케닐세팔로 스포린은 다음과 같은 반응공정에 따라 제조한다.-
公开(公告)号：KR102220428B1
公开(公告)日：2021-02-25
申请号：KR1020180092447
申请日：2018-08-08
Applicant: 한국과학기술연구원
IPC: C07D401/04 , A61K31/443 , A61K31/506 , C07D409/04 , A61P25/28
Abstract: 본발명은피리딘유도체및/또는 SHIP2 억제제로서의용도에관한것으로서, 화학식 I의피리딘유도체또는이의약학적으로허용가능한각각의염, 이들화합물의제조방법, 그리고이들화합물이유효성분으로함유된약학조성물에관한것이다. 상기한피리딘유도체및 이의약학적으로허용가능한염은 SHIP2와관련된질환예를들면알츠하이머성치매, 고혈압, 암, 당뇨등의치료용약제로유용하다.
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公开(公告)号：KR102039578B1
公开(公告)日：2019-11-01
申请号：KR1020170066800
申请日：2017-05-30
Applicant: 한국과학기술연구원 , 가천대학교 산학협력단 , 고려대학교 산학협력단
IPC: C07D311/30 , A61K31/352 , A61K36/282
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