1-ethyl-6-fluoro-1,4-dihydro- 7-(2,6-dimethyl-4-pyridinyl)-4-oxo

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546156, A61K 3147, C07D21518

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active

046983503

ABSTRACT:
1-Ethyl-6-fluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinoline carboxylic acid (Win 52,522) or salt thereof, a highly potent antibacterial agent, is prepared by nitrating the corresponding 6-desfluoro compound (Win 35,439) to produce the corresponding 6-nitro compound, reducing the latter compound to produce the corresponding 6-amino compound and converting the 6-amino via its diazonium salt to said 6-fluoro compound (Win 52,522). Comparative in vitro and in vivo antibacterial test data are provided to demonstrate the uniqueness of Win 52,522 as a highly potent antibacterial agent having a broad spectrum of antimicrobial activity.

REFERENCES:
patent: 3753993 (1973-08-01), Lesher et al.
patent: 3907808 (1975-09-01), Lesher
patent: 4146719 (1979-03-01), Irikura
patent: 4292317 (1981-09-01), Pesson
patent: 4533735 (1985-08-01), Walter
patent: 4554352 (1985-11-01), Ranken
Albrecht-Progress in Drug Research 21, pp. 35-45, 1977.
Morrison, Organic Chemistry, 2nd Edition, pp. 824 and 825, (1970) Allyn and Bacon.

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