7H-PYRIDO(3,2,1-IJ) (2,1)BENZOXAZIEN DERIVATIVE

NEW MATERIAL:The derivative of formula I (R is H or lower alkyl) and its salt. EXAMPLE:9,10-Difluoro-7-oxo-1,2-dihydro-7H-pyrido[3,2,1-ij][2,1]benzox azine-6- carboxylic acid. USE:An intermediate for a compound of formula II (X is N-substituted 5- to 7-membered saturated cyclic amine) useful as a th...

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Hauptverfasser: WATABE MAYUMI, SAKAE MASATOSHI, SABATO TAKAAKI, KATSURADA MASANORI, NISHIGAKI SADAO
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creator WATABE MAYUMI
SAKAE MASATOSHI
SABATO TAKAAKI
KATSURADA MASANORI
NISHIGAKI SADAO
description NEW MATERIAL:The derivative of formula I (R is H or lower alkyl) and its salt. EXAMPLE:9,10-Difluoro-7-oxo-1,2-dihydro-7H-pyrido[3,2,1-ij][2,1]benzox azine-6- carboxylic acid. USE:An intermediate for a compound of formula II (X is N-substituted 5- to 7-membered saturated cyclic amine) useful as a therapeutic agent for infection with Gram-negative and Gram-positive bacteria. PREPARATION:The objective compound of formula I can be produced by treating a compound of formula III with ethoxymethylenemalonic acid diethyl ester to obtain a compound of formula IV, converting the compound into an OH-protected compound of formula V by treating with acetic anhydride, heating the product together with a polyphosphoric acid ethyl ester, treating the resultant compound of formula VI with a halogenation agent, deprotecting by alkali treatment to obtain a compound of formula VII and treating the compound with an acid to effect intramolecular cyclization reaction.
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title 7H-PYRIDO(3,2,1-IJ) (2,1)BENZOXAZIEN DERIVATIVE
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