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:
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:
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.