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公开(公告)号：KR1019920006344A
公开(公告)日：1992-04-27
申请号：KR1019900015167
申请日：1990-09-25
Applicant: 한국화학연구원
IPC: C07D401/04
Abstract: 내용 없음
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公开(公告)号：KR1020060020082A
公开(公告)日：2006-03-06
申请号：KR1020040068822
申请日：2004-08-31
Applicant: 한국화학연구원
IPC: C07D213/73
CPC classification number: C07D213/73 , C07D213/77
Abstract: 본 발명은 2-아미노피리딘 유도체를 제조하는 방법에 관한 것으로, 본 발명에 따라 3-치환-2,5,6-트리플루오르피리딘을 히드라진 일수화물과 반응시켜 히드라지노기를 도입시킨 후, 바로 수소로 환원반응 시키거나, 또는 히드라지노기를 탈리시킴으로써 불소 치환기 하나를 제거하고 다시 히드라진 일수화물과 반응시켜 히드라지노기를 도입시켜 수소로 환원반응 시키는 단계를 포함하는 2-아미노-3-플루오르피리딘 유도체를 제조하는 방법은, 저가의 원료물질들을 사용하여 산업적 적용이 용이한 공정을 통해 2-아미노피리딘 유도체를 고순도로 제조할 수 있으므로, CCR(cellular chemokine receptor: 세포화학수용체)5 모듈레이터(modulator)의 제조 뿐만 아니라 감염증 치료제(anti-infective agents)의 제조 등에 유용하게 활용될 수 있다.
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公开(公告)号：KR100463993B1
公开(公告)日：2004-12-30
申请号：KR1020010088822
申请日：2001-12-31
Applicant: 한국화학연구원
IPC: C07D471/04
Abstract: PURPOSE: Quinolone type antimicrobial agents and a preparation process thereof are provided, which compounds have improved antimicrobial activity and wide range of antimicrobial spectrum. CONSTITUTION: Quinolone type antimicrobial agents are represented by the formula 1, wherein R1 is C1-4 alkyl, halogen substituted or unsubstituted phenyl, or halogen substituted or unsubstituted C3-6 cycloalkyl; R2 is hydrogen, amino or C1-4 alkyl; R5 is hydrogen, C1-4 alkyl, C1-4 alkyl substituted or unsubstituted amino, or C1-4 alkyl substituted or unsubstituted aminomethyl or aminoethyl; W is nitrogen, CH or CY; Y is halogen, or halogen substituted or unsubstituted C1-4 alkyl or C1-4 alkoxy; and Pyr is 2-, 3- or 4-pyridyl, provided that W and R1 form COCH2CH(CH3), CCH2CH2CH(CH3) or CSCH2CH(CH3) together when W is CH. A process for preparing the quinolone type antimicrobial agents comprises condensation reacting a compound of the formula 2 with a compound of the formula 3, wherein X is halogen; and HA is hydrogen chloride or trifluoroacetic acid.
Abstract translation: 目的：提供喹诺酮类抗菌剂及其制备方法，该化合物具有改善的抗微生物活性和广泛的抗微生物谱。 构成：喹诺酮类抗微生物剂由式1表示，其中R 1是C 1-4烷基，卤素取代或未取代的苯基或卤素取代或未取代的C 3-6环烷基; R2是氢，氨基或C1-4烷基; R5为氢，C1-4烷基，C1-4烷基取代或未取代的氨基或C1-4烷基取代或未取代的氨基甲基或氨基乙基; W是氮，CH或CY; Y是卤素或卤素取代或未取代的C 1-4烷基或C 1-4烷氧基; 并且Pyr是2-，3-或4-吡啶基，条件是当W是CH时，W和R1一起形成COCH2CH（CH3），CCH2CH2CH（CH3）或CSCH2CH（CH3）。 制备喹诺酮类抗微生物剂的方法包括使式2化合物与式3化合物缩合反应，其中X是卤素; HA是氯化氢或三氟乙酸。
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公开(公告)号：KR1020030058401A
公开(公告)日：2003-07-07
申请号：KR1020010088829
申请日：2001-12-31
Applicant: 한국화학연구원
IPC: C07D401/02
Abstract: PURPOSE: Pyrolidinyl derivatives used as substituents for preparing antimicrobial agents are provided, which compounds confer improved antimicrobial activity and wide range of antimicrobial spectrum to quinolone type, quinolizine type, carbapenem type, penem type or cephalosporin type derivatives when coupled with the antimicrobial agents. CONSTITUTION: Pyrolidinyl derivatives are represented by the formulas 1a, 1b and 1c, wherein R1 is hydrogen, C1-5 alkyl, C1-5 alkyl substituted or unsubstituted amino, or C1-5 alkyl substituted or unsubstituted aminomethyl; R2, R3, R4 and R5 are hydrogen, halogen, C1-5 alkyl, amino, nitro or cyano; HX is hydrochloric acid or trifluoroacetic acid; and n is 0, 2 or 3.
Abstract translation: 目的：提供用作制备抗微生物剂的取代基的吡咯烷基衍生物，当与抗微生物剂偶联时，该化合物赋予喹诺酮型，喹嗪类，碳青霉烯类，penem型或头孢菌素型衍生物更好的抗菌活性和广泛的抗菌谱。 构成：吡咯烷基衍生物由式1a，1b和1c表示，其中R1是氢，C1-5烷基，C1-5烷基取代或未取代的氨基或C1-5烷基取代或未取代的氨基甲基; R 2，R 3，R 4和R 5是氢，卤素，C 1-5烷基，氨基，硝基或氰基; HX是盐酸或三氟乙酸; 并且n为0,2或3。
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Patent Agency Ranking
公开(公告)号：KR1020030058394A
公开(公告)日：2003-07-07
申请号：KR1020010088822
申请日：2001-12-31
Applicant: 한국화학연구원
IPC: C07D471/04
Abstract: PURPOSE: Quinolone type antimicrobial agents and a preparation process thereof are provided, which compounds have improved antimicrobial activity and wide range of antimicrobial spectrum. CONSTITUTION: Quinolone type antimicrobial agents are represented by the formula 1, wherein R1 is C1-4 alkyl, halogen substituted or unsubstituted phenyl, or halogen substituted or unsubstituted C3-6 cycloalkyl; R2 is hydrogen, amino or C1-4 alkyl; R5 is hydrogen, C1-4 alkyl, C1-4 alkyl substituted or unsubstituted amino, or C1-4 alkyl substituted or unsubstituted aminomethyl or aminoethyl; W is nitrogen, CH or CY; Y is halogen, or halogen substituted or unsubstituted C1-4 alkyl or C1-4 alkoxy; and Pyr is 2-, 3- or 4-pyridyl, provided that W and R1 form COCH2CH(CH3), CCH2CH2CH(CH3) or CSCH2CH(CH3) together when W is CH. A process for preparing the quinolone type antimicrobial agents comprises condensation reacting a compound of the formula 2 with a compound of the formula 3, wherein X is halogen; and HA is hydrogen chloride or trifluoroacetic acid.
Abstract translation: 目的：提供喹诺酮类抗微生物剂及其制备方法，该化合物具有改善的抗菌活性和广泛的抗菌谱。 组成：喹诺酮类抗微生物剂由式1表示，其中R1为C1-4烷基，卤素取代或未取代的苯基或卤素取代或未取代的C3-6环烷基; R2是氢，氨基或C1-4烷基; R5是氢，C1-4烷基，C1-4烷基取代或未取代的氨基或C1-4烷基取代或未取代的氨基甲基或氨基乙基; W是氮，CH或CY; Y是卤素，或卤素取代或未取代的C 1-4烷基或C 1-4烷氧基; 并且Pyr是2-，3-或4-吡啶基，条件是当W是CH时，W和R 1一起形成COCH 2 CH（CH 3），CCH 2 CH 2 CH（CH 3）或CSCH 2 CH（CH 3）。 制备喹诺酮型抗微生物剂的方法包括使式2化合物与式3化合物缩合反应，其中X为卤素; HA是氯化氢或三氟乙酸。
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公开(公告)号：KR100274315B1
公开(公告)日：2000-12-15
申请号：KR1019980011452
申请日：1998-04-01
Applicant: 한국화학연구원
IPC: C07D487/10
Abstract: PURPOSE: Provided are the novel spirohydantoin compounds inhibiting the bio-synthesis of cholesterol thereby lowering the concentration of the blood lipids. CONSTITUTION: The novel compounds are represented by the chemical formula 1, where R1 is hydrogen, C1-4 alkyl or C3-4 cycloalkyl group; R2 is hydrogen, halogen or nitro group; A is carbon or nitrogen; m is 0 or 1; n is 1 or 2. The synthetic process comprises the steps of: decarboxylation of N-benzyl-N-ethoxycarbonylmethyl-β-alaninate(general formula II) with 6-12N concentrated HCl to obtain the compound of general formula III; reacting the compound III in ethanol or ethanol/water solution, with potassium or sodium cyanide and ammonium carbonate at 50-90deg.C for 10-48 hours to obtain compound of general formula IV; reacting the compound IV with diethoxy propyl bromide in the presence of bases such as sodium hydride, sodium ethoxide or potassium t-buthoxide to make the compound of general formula V-1; introducing R1 group to the amide group of the compound V-1 in the presence of base such as sodium hydride to make the compound of general formula V-2; converting the acetal group in the compounds V-1 and V-2 to aldehyde group in the presence of hydrochloric acid or p-toluenesulfonic acid to make the compound of general formula VI; carrying out aldol condensation of the compound VI with ethylacetoacetate in the presence of base such as n-butyl lithium to obtain the compound of general formula VII; converting β-carbonyl group in the compound VII to alcohol by reacting with triethylborane, sodium borohydride or sodium borocyanohydride in THF to make the compound of general formula VIII and lactonising to the final compound of the chemical formula 1 after hydrolysis of the compound VIII with base or acid.
Abstract translation: 目的：提供抑制胆固醇生物合成的新型螺乙内酰脲化合物，从而降低血脂浓度。 构成：新化合物由化学式1表示，其中R1是氢，C1-4烷基或C3-4环烷基; R2是氢，卤素或硝基; A是碳或氮; m为0或1; n为1或2.合成方法包括以下步骤：用6-12N浓HCl将N-苄基-N-乙氧基羰基甲基-β-丙氨酸酯（通式II）脱羧，得到通式Ⅲ化合物; 使化合物III在乙醇或乙醇/水溶液中与氰化钾或氰化钠和碳酸铵在50-90℃反应10-48小时，得到通式Ⅳ化合物; 在碱如氢化钠，乙醇钠或叔丁醇钾存在下使化合物IV与二乙氧基丙基溴反应，制得通式V-1的化合物; 在碱如氢化钠存在下，将R1基团引入到化合物V-1的酰胺基上，得到通式V-2的化合物; 在盐酸或对甲苯磺酸的存在下将化合物V-1和V-2中的缩醛基转化成醛基，得到通式VI的化合物; 在碱例如正丁基锂存在下进行化合物VI与乙酰乙酸乙酯的醛醇缩合，得到通式Ⅶ化合物; 通过与THF中的三乙基硼烷，硼氢化钠或硼氢化钠在THF中反应，将化合物VII中的β-羰基转化成醇，以制备通式VIII的化合物，并在化合物VIII与碱水解后将其内酰化至化学式1的最终化合物 或酸。
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公开(公告)号：KR100263023B1
公开(公告)日：2000-08-01
申请号：KR1019980011451
申请日：1998-04-01
Applicant: 한국화학연구원
IPC: C07D215/233
Abstract: PURPOSE: Provided are the quinolone derivatives of chemical formula (I) and (II) which show the activity of lowering blood lipids concentration by inhibiting the functions of HMG-CoA reductase. CONSTITUTION: In the chemical formula (I) and (II), X is CY and N (where Y is hydrogen, halogen, C1-2 alkyl); R1 is C1-4 alkyl, C3-4 cycloalkyl or phenyl group substituted with one or more fluorine atom. Quinolone-3-ethenyl-3'β5'β-dihydroxypentanoic acid (chemical formula I) is prepared by the steps consisting of: converting the acid (III) to aldehyde; converting this aldehyde to enoic acid by the Wittig reaction; changing this acid into the corresponding aldehyde; condensing the aldehyde with ethyl acetoacetate to have the product of chemical formula I, with racemic 5' hydroxy group and reducing the product into the chemical formula II. The compounds and their pharmaceutically acceptable salts lower the blood lipids by inhibition of the HMG-CoA reductase.
Abstract translation: 目的：提供化学式（I）和（II）的喹诺酮衍生物，其通过抑制HMG-CoA还原酶的功能来显示降低血脂浓度的活性。 构成：在化学式（I）和（II）中，X是CY和N（其中Y是氢，卤素，C 1-2烷基）; R1是被一个或多个氟原子取代的C1-4烷基，C3-4环烷基或苯基。 喹诺酮-3-乙烯基-3'β5'β-二羟基戊酸（化学式I）通过以下步骤制备：将酸（III）转化为醛; 通过Wittig反应将该醛转化为烯酸; 将该酸变成相应的醛; 将醛与乙酰乙酸乙酯缩合成具有化学式I的产物，与外消旋的5'羟基反应，并将产物还原成化学式II。 化合物及其药学上可接受的盐通过抑制HMG-CoA还原酶降低血脂。
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公开(公告)号：KR1019990079063A
公开(公告)日：1999-11-05
申请号：KR1019980011451
申请日：1998-04-01
Applicant: 한국화학연구원
IPC: C07D215/233
Abstract: 본 발명은 콜레스테롤의 생합성에 관여하는 효소들 중, 특히 HMG-Co A 환원효소의 작용을 저해하는, 3위치에 에테닐-3'β,5'β-디히드록시펜타노익산이 도입된 하기 일반식(I)의 퀴놀론 유도체 및 3위치에 에틸-3'β,5'β-디히드록시펜타노익산이 도입된 하기 일반식(II)의 퀴놀론 유도체, 및 이들의 제조방법에 관한 것으로, 본 발명에 따라 제조된 퀴놀론-3-에틸 또는 에테닐-3'β,5'β-디히드록시펜타노익산 유도체는 콜레스테롤 합성효소 저해효과가 우수하여 혈중 지질농도를 저하시키는데 유리하다:
상기 식에서,
X는 CY 또는 N이고(이때, Y는 수소, 할로겐, C
1-4 알콕시 또는 C
1-4 알킬이고);
R
1 은 C
1-4 알킬, C
3-4 사이클로알킬 또는 하나 이상의 불소로 치환된 페닐이다.-
公开(公告)号：KR1019960003610B1
公开(公告)日：1996-03-20
申请号：KR1019910025883
申请日：1991-12-31
Applicant: 한국화학연구원
IPC: C07D471/04
Abstract: The quinolone carboxylic acid derivs. of formula (I) are prepd. by reacting a cpd. of formula(II) with a cpd. of formula(III) in the reactive solvent i.e. acetonitrile, dimethyl formamide, dimethyl sulfoxide, pyridine, water and/or alcohol in the presence of a base i.e. calcium carbonate, potassium carbonate or triethyl amine at 20˜200deg. C for 1-24hr. In the formulas, R1, R2 and R3 are each H, halogen or lower alkyl; R4 is H, lower alkyl, benzyl or ethoxy carbonyl; R5 is H, Cl, methyl or amino; R6 is lower alkyl, cyclopropyl or phenyl; X is N, lower alkyl or methine; Y is halogen, mecyl or tocyl. The derivs. (I) have a broad antibacterial activity against gram negative and positive bacteria.
Abstract translation: 喹诺酮羧酸衍生物。 式（I）的化合物是制备的。 通过反应cpd。 的式（II）与cpd。 （III）在反应性溶剂即乙腈，二甲基甲酰胺，二甲基亚砜，吡啶，水和/或醇中，在碱的存在下，即碳酸钙，碳酸钾或三乙胺，存在20〜200℃。 C为1-24小时。 在式中，R 1，R 2和R 3各自为H，卤素或低级烷基; R4是H，低级烷基，苄基或乙氧基羰基; R5是H，Cl，甲基或氨基; R6是低级烷基，环丙基或苯基; X是N，低级烷基或次甲基; Y是卤素，十八烷基或十八烷基。 派生词。 （I）对革兰氏阴性和阳性细菌具有广泛的抗菌活性。
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