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Title:
1,4-DIHYDRO-4-OXONAPHTHYRIDINE DERIVATIVE OR ITS SALT
Document Type and Number:
Japanese Patent JP2630566
Kind Code:
B2
Abstract:

PURPOSE: To obtain 1,4-dihydro-4-oxonaphthyridine derivative of a specific formula useful as a naphthyridine-based synthetic antibacterial agent showing a strongly antibacterial action on gram-positive and gram negative bacteria, especially on antibiotic-resistant bacterium.
CONSTITUTION: The compound of containing I [R1 is H or a carboxylprotecting group; R2 is a halogen or a (substituted) cyclic amino; R3 is a (substituted) aryl; A is a lower alkylene] such as 2-(2,6-dichloro-5-fluoronicotinoyl)-3-(3- fluorobenzylamino)acrylic acid ethyl ester, etc. The compound is preferably obtained by reacting a compound of formula II with ethyl orthoformate in acetic anhydride, and then with an amine to give a compound of formula III, subjecting the compound of formula III to ring closure reaction and reacting the prepared compound of formula IV with a cyclic amine in the presence of an inert solvent such as benzene.


Inventors:
NARITA HIROKAZU
KONISHI YOSHINORI
NITSUTA JUN
TAKAGI HIROYASU
IINO FUMIHIKO
KOBAYASHI JUNKO
SAIKAWA ISAMU
Application Number:
JP21801594A
Publication Date:
July 16, 1997
Filing Date:
August 19, 1994
Export Citation:
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Assignee:
TOYAMA KAGAKU KOGYO KK
International Classes:
A61K31/435; A61K31/495; A61P31/04; C07D471/04; (IPC1-7): C07D471/04
Domestic Patent References:
JP717642B2