这里有全文
http://v3.espacenet.com/publicationDetails/biblio?CC=JP&NR=4364185A&KC=A&FT=D&date=19921216&DB=EPODOC&locale=en_EP
Publication number: JP4364185 (A)
Publication date: 1992-12-16
Inventor(s): HAYAKAWA ISAO; SHINKO SEIGO; YOKOHAMA SHUICHI; IMAMURA MASAZUMI; SAKANO KATSUICHI
Applicant(s): DAIICHI SEIYAKU CO
Classification:
- international: A61K31/535; A61P31/04; C07D498/06; A61K31/535; A61P31/00; C07D498/00; (IPC1-7): A61K31/535; C07D498/06
- European:
Application number: JP19910078141 19910118
Priority number(s): JP19910078141 19910118; JP19860016496 19860128; JP19850134712 19850620
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Also published as:
JP7047592 (B)
JP2008845 (C)
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Abstract of JP 4364185 (A)
PURPOSE:To obtain a new compound useful as an antimicrobial agent, having low toxicity. CONSTITUTION:S-(-)-9-Fluoro-3-methyl-10-(4-methyl or ethyl-1-piperazinyl)-7- oxo-2,3-dihydro-7H-pyrido[1,2,3-de[[1,4]benzoxazine-6-carboxulic acid. This compound is obtained by subjecting a 3-alkyl-7,8-dihalogeno-1,4-benzoxazine derivative shown by formula I and a cyclic amino acid shown by formula II to amide bond reaction to give a diastereomer mixture shown by formula III. The mixture is subjected to fractional crystallization, separated and the product is hydrolyzed to give a 3S-7,8-dihalogeno-3-alkyl-1,4-benzoxazine shown by formula IV, which is allowed to react with a lower alkoxymethylenemalonic acid di-lower alkyl ester and the product is reacted with a polyphosphoric acid, etc., under heating and the product is reacted with an N-lower alkylpiperazine. |