Preparation of 2,7-diazabicyclo[3.3.0]octanes

US5071999A · kind A · utility

Assignee

• BAYER HEALTHCARE LLC · DE

Inventors

• Thomas Schenke · Odenthal, DE
• Uwe Petersen · Leverkusen, DE

Key dates

• Filing date: Apr 10, 1990
• Grant date: Dec 10, 1991
• Expiry date: Apr 10, 2010

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D513/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

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, PA0 R.sup.4 additionally denotes halogen, PA0 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, or PA0 R.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, PA0 excluding 2,7-diazabicyclo[3.3.0]octane. Also their preparation by the reaction ##STR2## Intermediates II are also new.