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公开(公告)号：KR1020000074954A
公开(公告)日：2000-12-15
申请号：KR1019990019241
申请日：1999-05-27
Applicant: 한국과학기술연구원
IPC: C07D413/14
Abstract: PURPOSE: Provided is an isooxazolyl methylene oxazolidinone derivative represented by the formula (I) which is superior in antibacterial activity. Also, a method for preparing the compound is provided. CONSTITUTION: An isooxazoly methylene oxazolidinone derivative is represented by the formula (I): wherein, R is hydrogen, alkyl, halogen such as bromine or chlorine, cyano, alkoxy, hydroxy, carboxy, carbamoyl, N,N'-dimethylcarbamoyl, carbamoyloxy, oxygen, sulfur, thiopene having more than one nitrogen atom, thiazole, aminothiazole, isothiazole, isooxazole, oxazole, tetrazole, 5 or 6-membered unsaturated heterocycle substituent of pyridine, alkyl, halogenalkoxy, benzene ring substituted with cyano or phenoxy group, pharmaceutically acceptable methanesulfonate, fumarate, bromate, citrate, phosphate, sulfate or amine not being salt. The isooxazoly methylene oxazolidinone derivative is prepared by reacting oxazolidine derivative represented by the formula (II) and isooxazole derivative represented by the formula (III) a using a reductant in the presence of a solvent.
Abstract translation: 目的：提供抗菌活性优异的由式（I）表示的异恶唑基亚甲基恶唑烷酮衍生物。 此外，提供了制备该化合物的方法。 构型：异恶唑基亚甲基恶唑烷酮衍生物由式（I）表示：其中R是氢，烷基，卤素如溴或氯，氰基，烷氧基，羟基，羧基，氨基甲酰基，N，N'-二甲基氨基甲酰基，氨基甲酰氧基， 氧，硫，具有多于一个氮原子的噻吩，噻唑，氨基噻唑，异噻唑，异恶唑，恶唑，四唑，吡啶，烷基，卤代烷氧基，被氰基或苯氧基取代的苯环的5或6元不饱和杂环取代基， 甲磺酸盐，富马酸盐，溴酸盐，柠檬酸盐，磷酸盐，硫酸盐或胺不是盐。 异恶唑亚甲基恶唑烷酮衍生物通过使用还原剂在溶剂存在下使式（II）表示的恶唑烷衍生物和由式（III）a表示的异恶唑衍生物反应来制备。
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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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Patent Agency Ranking
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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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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