8-aminopyrido(1,2,3-de)(1,4)banzoxazine derivative

Abstract

Abstract NEW MATERIAL:A compound of formulaI[R<3> is H, lower alkyl; R<10> is mono- or disubstituted or cyclic amine, where these substituents may contain hetero atoms or may be substituted with hydroxyl, lower alkyl, lower alkoxy or amino; X is halogen]and its salts. EXAMPLE:8-Amino-9-fluoro-3-methyl-10- ( 4-methyl-1-piperazinyl ) -7-oxo-2, 3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid. USE:Antibacterial: it is effective against gram-positive and -negative bacteria including Pseudomonas areuginosa. PREPARATION:A compound of formula II in a polar solvent such as dimethyl sulfoxide or sulfolane is heated with an amine of R<10>H at room temperature to 200 deg.C, preferably 70-150 deg.C for 30min to 48hr to give the compound of formula I.

Inventors

• 👤 Isao Hayakawa
• 👤 Yoshiaki Tanaka

Bibliographic Details