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Details for Patent: 5,391,763

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Details for Patent: 5,391,763

Title: 3-aza-bicyclo[3.1.0]hexanes which are intermediates for anti-bacterial azabicyclo quinolone carboxylic acids
Abstract:Quinolone carboxylic acids 7 -substituted by azabicyclo groups have antibacterial activity.
Inventor(s): Brighty; Katherine E. (Groton, CT)
Assignee: Pfizer Inc. (New York, NY)
Filing Date:Aug 26, 1993
Application Number:08/088,999
Claims:1. A compound of the formula ##STR17## wherein Y.sup.2 is hydrogen, benzyl, or benzyloxycarbonyl, and R.sup.15 is carboxyl, hydroxymethyl, CHO, CH.sub.2 NR.sup.11 R.sup.12 or NR.sup.11 R.sup.12 wherein R.sup.11 is hydrogen, methyl, or ethyl, and R.sup.12 is hydrogen, C.sub.1 -C.sub.6 acyl, C.sub.2 -C.sub.6 alkoxycarbonyl, optionally substituted benzyloxycarbonyl, aryloxycarbonyl, silyl, trityl, tetrahydropyranyl- vinyloxycarbonyl, O-nitrophenylsulfonyl, diphenylphosphonyl, p-toluenesulfonyl, or benzyl.

2. A compound of the formula ##STR18## wherein Y.sup.2 is hydrogen, benzyl, or benzyloxycarbonyl, R.sup.18 is methyl, cyano, hydroxymethyl, or CH.sub.2 NR.sup.11 R.sup.12, and

R.sup.19 is methyl, carboxyl, hydroxymethyl, CHO, hydroxymethyl tetrahydropyranyl ether, CH.sub.2 NR.sup.11 R.sup.12, or NR.sup.11 R.sup.12, wherein R.sup.11 is hydrogen, methyl or ethyl and R.sup.12 is hydrogen, C.sub.1 -C.sub.6 acyl, C.sub.2 -C.sub.6 alkoxycarbonyl, optionally substituted benzyloxycarbonyl, aryloxycarbonyl, silyl, trityl, tetrahydropyranyl, vinyloxycarbonyl, o-nitrophenylsulfonyl, diphenylphosphonyl, p-toluenesulfonyl, or benzyl, with the proviso that when R.sup.19 is methyl and Y.sup.2 is hydrogen, then R.sup.18 is not cyano.

3. A compound of the formula ##STR19## wherein Y.sup.2 is hydrogen, benzyl, or benzyloxycarbonyl, R.sup.18 is methyl, hydroxymethyl, or CH.sub.2 NR.sup.11 R.sup.12, and

R.sup.19 is methyl, carboxyl, hydroxymethyl, CHO, hydroxymethyl tetrahydropyranyl ether, CH.sub.2 NR.sup.11 R.sup.12, or NR.sup.11 R.sup.12, wherein R.sup.11 is hydrogen, methyl or ethyl and R.sup.12 is hydrogen, C.sub.1 -C.sub.6 acyl, C.sub.2 -C.sub.6 alkoxycarbonyl, optionally substituted benzyloxycarbonyl, aryloxycarbonyl, silyl, trityl, tetrahydropyranyl, vinyloxycarbonyl, o-nitrophenylsulfonyl, diphenylphosphonyl, p-toluenesulfonyl, or benzyl.
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