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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：KR1019930007811B1
公开(公告)日：1993-08-20
申请号：KR1019900016941
申请日：1990-10-23
Applicant: 한국화학연구원
IPC: C07D501/24
Abstract: 3-Vinylcephem derivatives of formula (I) which are useful as an oral antibiotics and it's intermediates were prepd. from 7- aminocephalosporin. In (I), R1=H or aralkanoyl as (A) or oxyimino substd. aralkanoyl or hetero aralkanoyl as (B), R2=Cl, Br, R3= phenyl or mono substd. phenyl or cyclohexadienyl, R4= 2- aminothiazolyl, R5= methylacetic acid or dimethylacetic acid. Cpd. (I) have better absorption and antibacterial activity against Gram negative bacteria for oral use than existing oral cephems.
Abstract translation: 可用作口服抗生素的式（I）的3-乙烯基头孢烯衍生物及其中间体是制备的。 来自7-氨基头孢菌素。 在（I）中，R 1 = H或芳烷酰基（A）或氧亚氨基。 芳烷酰基或杂芳烷酰基作为（B），R 2 = Cl，Br，R 3 =苯基或单子取代。 苯基或环己二烯基，R 4 = 2-氨基噻唑基，R 5 =甲基乙酸或二甲基乙酸。 CPD。 （I）对口腔使用革兰氏阴性细菌的吸收和抗菌活性比现有的口腔流行病好。
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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：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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Patent Agency Ranking
公开(公告)号：KR1019910016759A
公开(公告)日：1991-11-05
申请号：KR1019900004181
申请日：1990-03-28
Applicant: 한국화학연구원
IPC: C07D498/04 , C07D498/06
Abstract: 내용 없음
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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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公开(公告)号：KR1019910003186B1
公开(公告)日：1991-05-22
申请号：KR1019890003657
申请日：1989-03-23
Applicant: 한국화학연구원
IPC: C07D403/04 , C07D401/04
Abstract: Quinolone derivs. of formula (I) are prepd. by a condensation reaction of a quinolinecarboxylic acid cpd. of formula (II) and a pyrroline cpd. of formula (III) in a solvent at 200 deg.C for 1-6 hrs. In the formulas, R1 and R2 each= H or C1-3 lower alkyl; R3= C1-3 lower alkyl; R4 and R5 each= H, halogen or amino gp. Pref. the solvent is H2O, alcohol, acetonitrile, dimethylformamide, dimethylsulfoxide, hexamethylphosphorictriamide, pyridine or picoline. Cpds. (I) have antibacterial activities.
Abstract translation: 喹诺酮衍生物。 式（I）的化合物是制备的。 通过喹啉羧酸cpd的缩合反应。 的式（II）和吡咯啉cpd。 的式（III）在溶剂中在200℃下反应1-6小时。 式中，R 1和R 2各自为H或C 1-3低级烷基; R3 = C1-3低级烷基; R4和R5各自为H，卤素或氨基。 县。 溶剂为H 2 O，醇，乙腈，二甲基甲酰胺，二甲基亚砜，六甲基磷酰三胺，吡啶或甲基吡啶。 CPDS。 （一）具有抗菌活性。
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