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公开(公告)号：KR1019940001770B1
公开(公告)日：1994-03-05
申请号：KR1019910018097
申请日：1991-10-15
Applicant: 한국화학연구원
IPC: C07D207/18
CPC classification number: C07D401/04 , C07D209/44 , C07D209/52 , Y02P20/55
Abstract: Azabicycloamine compounds and their salts of formula (I) are prepared. In the formula (I), R=H or amine protecting groups; R1,R2=H, lower alkyl, acyl, substituted (or unsubstituted) benzoyl, or naphtoyl, alkoxycarbonyl or substituted (or unsubstituted) benzyloxycarbonyl; n = 1-4. (I) are useful as intermediates in the preparation of antibacterial quinolone carboxylic acid derivatives, cephalosporin antibiotics and other drugs.
Abstract translation: 制备氮杂双环胺化合物及其式（I）的盐。 在式（I）中，R = H或胺保护基; R 1，R 2 = H，低级烷基，酰基，取代的（或未取代的）苯甲酰基或萘甲酰基，烷氧基羰基或取代的（或未取代）苄氧羰基; n = 1-4。 （I）可用作制备抗菌喹诺酮羧酸衍生物，头孢菌素抗生素等药物的中间体。
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公开(公告)号：KR1019910009331B1
公开(公告)日：1991-11-11
申请号：KR1019890015204
申请日：1989-10-23
Applicant: 한국화학연구원
IPC: C07D487/04
CPC classification number: C07D471/04 , C07D487/04
Abstract: Diazabicycloamine derivs. of formula (I) and their salts are new. In (I), m = 1-3; n = 1-2; and R1, R2 = H or lower alkyl. Also claimed is the preparation of (I) which comprises e.g. reacting tetrakis(halomethyl)ethylene (halo = Cl, Br or I) with NH3 to form (I) in which m and n = 1 and R1 and R2 = H. (I) is e.g. 3,7-diazabicyclo(3.3.0)oct-1(5)ene or 3,8-diazabicyclo(4.3.0)non-1(6)-ene. Cpd. (I) is used for mfg. new quinolone antibiotics (claimed), with high antibacterial activity against Gram negative and Gram positive bacteria and improved antibacterial activity against methicillin resistant Staphylococcus aureus compared to ofloxacin, norfloxacin and ciprofloxacin. The quinolone are used for treating urethritis. (I) is also used for the prepn. of cephalosporins. cpds.
Abstract translation: 二氮杂双环胺衍生物。 的式（I）及其盐是新的。 在（I）中，m = 1-3; n = 1-2; 和R 1，R 2 = H或低级烷基。 还要求保护的是（I）的制备，其包括例如 使四（卤代甲基）乙烯（卤代= Cl，Br或I）与NH 3反应形成其中m和n = 1且R 1和R 2 = H的（I）。 3,3-二氮杂双环（3.3.0）辛-1（5）烯或3,8-二氮杂双环（4.3.0）非-1（6）烯。 CPD。 （I）用于制造。 与氧氟沙星，诺氟沙星和环丙沙星相比，新型喹诺酮类抗生素（要求保护）对革兰氏阴性和革兰氏阳性菌具有较高的抗菌活性，对耐甲氧西林金黄色葡萄球菌的抗菌活性更好。 喹诺酮用于治疗尿道炎。 （I）也用于制备。 的头孢菌素。 国家方案文件。
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公开(公告)号：KR1019910009330B1
公开(公告)日：1991-11-11
申请号：KR1019890015202
申请日：1989-10-23
Applicant: 한국화학연구원
IPC: C07D487/04
CPC classification number: C07D471/04 , C07D487/04
Abstract: Quinolone derivs. of formula (I) and their acid addn. salts are new. In (I), X = C-H, C-F N; Z = H, halo or NH2; R1 = H or a cation; R2 = C1-4 (halo)hlkyl or hydroxyalkyl, or vinyl, C3-6 cycloalkyl or fluorophenyl; R3 = H, lower alkyl or formyl; m = 1- 3; n = 1 or 2. Also claimed is preparation of (I) which comprises e.g. condensing the corresponding quinolone derivative having a leaving gp. in the 7-position with a diazabicycloamine. (I) have improved and wider range of antibacterial activity against Gram positive and Gram negative bacteria than existing quinolone antibacterial agents, esp. norfloxacin, ciprofloxacin and ofloxacin. (I) have good antibacterial activity against methicillin resistant bacteria.
Abstract translation: 喹诺酮衍生物。 的式（I）和它们的酸加成。 盐是新的。 在（I）中，X = C-H，C-F N; Z = H，卤素或NH 2; R1 = H或阳离子; R2 = C1-4（卤代）烷基或羟基烷基，或乙烯基，C3-6环烷基或氟苯基; R3 = H，低级烷基或甲酰基; m = 1- 3; n = 1或2.还要求保护的是（I）的制备。 冷凝具有离去gp的相应喹诺酮衍生物。 在7-位与二氮杂双环胺。 （I）比现有的喹诺酮类抗菌药物具有改善和更广泛的抗革兰氏阳性和革兰氏阴性菌的抗菌活性。 诺氟沙星，环丙沙星和氧氟沙星。 （I）对耐甲氧西林细菌具有良好的抗菌活性。
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Patent Agency Ranking
公开(公告)号：KR1019940002953B1
公开(公告)日：1994-04-09
申请号：KR1019910006267
申请日：1991-04-19
Applicant: 한국화학연구원
IPC: C07D401/14
Abstract: An organic acid salt of quinolone carboxylic acid or its hydrate, of formula (I) is new. The cpd. (I) is prepd. by adding the org. acid to the quinolone carboxylic acid dervs. cpd. of formula (II) in the solvent comprising C1-4 haloalkane, C1-3 lower alcohol or their mixt. or water. In the formulas, X is N or C-Y, Y= H, F or CH3; R1 is C1-6 alkyl, hydroxy alkyl, vinyl, or C3-6 cycloalkyl or F-substd. phenyl; R2 is H, CH3, ethyl or 2-hydroxy ethyl; m is 1-3; n is 1-2; Z is H, amino, halogen or CH3; A is lactic acid, ascorbic acid, maleic acid, malonic acid, glutamic acid, cytric acid, fumaric acid, paratoluene sulfonic acid, acetic acid, propionic acid, or tartaric acid.
Abstract translation: 式（I）的喹诺酮羧酸或其水合物的有机酸盐是新的。 cpd。 （I）是prepd。 通过添加组织。 酸对喹诺酮羧酸衍生物。 CPD。 （II）的溶剂在包含C 1-4卤代烷烃，C 1-3低级醇或其混合物的溶剂中。 或水。 在该式中，X是N或C-Y，Y = H，F或CH 3; R 1是C 1-6烷基，羟基烷基，乙烯基或C 3-6环烷基或F-杂原子。 苯基; R2是H，CH3，乙基或2-羟基乙基; m为1-3; n为1-2; Z是H，氨基，卤素或CH 3; A是乳酸，抗坏血酸，马来酸，丙二酸，谷氨酸，麦芽酸，富马酸，对甲苯磺酸，乙酸，丙酸或酒石酸。
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公开(公告)号：KR1019930008224B1
公开(公告)日：1993-08-27
申请号：KR1019910003933
申请日：1991-03-12
Applicant: 한국화학연구원
IPC: C07D207/20
CPC classification number: Y02P20/55
Abstract: Pyrolidine derivs. of formula (I) and their acid salts are prepd. In (I), R1=H or lower alkyl (C1-4), R2, R3=H, lower alkyl (C1-3), cycloalkyl, or -OH, and n = 1 or 2. The cpds. of formula (II) are reacted with triethyl phosphonoacetate or ethyl bromoacetate triphenyl phosphonic acid in the presence of strong base to give cpds. of formula (III) which have exo double bond. In cpds. (III), nitrogen protective group is subtd. with ethoxy carbonyl group and then ester is reduced to give alcoholic cpds. These cpds. are converted to methane sulfonyl derivs, and NH(R2R3) is subtd. to give cpds. (VII). Cpds. (VII) are hydrolyzed to give cpds. (I). Cpds. (I) are useful as the intermediates in the prepn. of quinolone or cephalosphorin antibiotics.
Abstract translation: 吡咯烷衍生物。 的式（I）化合物及其酸式盐是制备的。 在（I）中，R1 = H或低级烷基（C1-4），R2，R3 = H，低级烷基（C1-3），环烷基或-OH，n = 1或2。 的式（II）化合物与膦酰基乙酸三乙酯或溴代乙酸乙酯三苯基膦酸在强碱存在下反应，得到cpds。 具有外键双键的式（III）化合物。 在cpds。 （III），氮保护基。 与乙氧基羰基，然后酯被还原以产生酒精cpds。 这些cpds。 转化为甲磺酰基衍生物，NH（R2R3）分解。 给cpds。 （VII）。 CPDS。 （VII）水解，得到cpds。 （一世）。 CPDS。 （I）可用作制剂中的中间体。 的喹诺酮或头孢菌素抗生素。
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公开(公告)号：KR1019930007901A
公开(公告)日：1993-05-20
申请号：KR1019910018097
申请日：1991-10-15
Applicant: 한국화학연구원
IPC: C07D207/18
Abstract: 본 발명은 다음 일반식(Ⅰ)의 표시되는 아자비시클로아민 화합물과 그의 제조방법에 관한 것으로, 더욱 상세하게는, 퀼놀론 카르복실산 항균제, 세팔로스포린 항생제 또는 다른 항생물질이나 다른 의약품의 측쇄용 중간체로 유용한 불포화 아자비시클로아민 화합물과 이들 화합물의 염 및 그의 제조방법에 관한 것이다.
상기 식에서, R은 수소원자 또는 아민보호기이고, R
1 , R
2 는 서로 같거나 다른 치환기로서, 수소원자, 저급알킬기, 아실기, 치환 또는 치환되지 않은 벤조일기 또는 나프토일기, 알콕시카르보닐기, 또는 치환 또는 치환되지 않은 벤질옥시카르보닐기이고, n은 1 내지 4의 정수이다.-
公开(公告)号：KR1019910007932A
公开(公告)日：1991-05-30
申请号：KR1019890015204
申请日：1989-10-23
Applicant: 한국화학연구원
IPC: C07D487/04
Abstract: 내용 없음
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