Preparation of 2,7-diazabicyclo(3.3.0)octanes
    71.
    发明授权
    Preparation of 2,7-diazabicyclo(3.3.0)octanes 失效
    制备2,7-二氮杂双环(3.3.0)辛烷

    公开(公告)号:US5177210A

    公开(公告)日:1993-01-05

    申请号:US748312

    申请日:1991-08-21

    摘要: 2,7-Diazabicyclo[3.3.0]octanes, suitable for 7-position substituents or antibacterially active quinolone carboxylic acids, of the formula ##STR1## in which R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.7 and R.sup.8 may be identical or different and in each case denote H, C.sub.1 -C.sub.5 -alkyl (optionally substituted by halogen, hydroxyl or C.sub.1 -C.sub.3 -alkoxy), C.sub.1 -C.sub.3 -alkoxycarbonyl or C.sub.6 -C.sub.12 -aryl,R.sup.4 additionally denotes halogen,R.sup.2 and R.sup.6 may be identical or different, denote H, C.sub.1 -C.sub.6 -alkyl, benzyl, C.sub.6 -C.sub.12 -aryl, C.sub.1 -C.sub.3 -alkanoyl, benzoyl or C.sub.1 -C.sub.5 -alkoxycarbonyl, orR.sup.2 and R.sup.3 together denote a bridge of the structure (CH.sub.2).sub.n, n=2-4, CH.sub.2 --CHOH--CH.sub.2, CH.sub.2 --S--CH.sub.2 or C(CH.sub.3).sub.2 --S--CH.sub.2,excluding 2,7-diazabicyclo[3.3.0]octane.Also their preparation by the reaction ##STR2## Intermediates II are also new.

    摘要翻译: 2,7-二氮杂双环[3.3.0]辛烷,其中R 1,R 3,R 4,R 5,R 7和R 8可以相同,其具有式(I)的7-位取代基或抗菌活性喹诺酮羧酸 或者不同,并且在每种情况下都表示H,C 1 -C 5 - 烷基(任选被卤素,羟基或C 1 -C 3 - 烷氧基取代),C 1 -C 3 - 烷氧基羰基或C 6 -C 12 - 芳基,R 4另外表示卤素,R 2和R 6可以 表示H,C 1 -C 6 - 烷基,苄基,C 6 -C 12 - 芳基,C 1 -C 3 - 烷酰基,苯甲酰基或C 1 -C 5 - 烷氧基羰基,或者R 2和R 3一起表示结构(CH 2) n,n = 2-4,CH2-CHOH-CH2,CH2-S-CH2或C(CH3)2-S-CH2,不包括2,7-二氮杂双环[3.3.0]辛烷。 此外,它们通过反应制备 + TR(I)+ CO 2 + H 2 O中间体II也是新的。