Toyama Chemical Co., Ltd.

Katsuji Ojima

Tamotsu Takamatsu

Taro Kiyoto

Kazuya Hayashi

Kyoko Taya

Minako Yotsuji

Kenji Yonezawa

Hironori Kotsubo

Hirohiko Yamamoto

Minoru Yamada

Shoichi Hamamoto

Hiroko Matsukura

Kazuko Takaoka

Junichi Mitsuyama

Kazuto Kunitani

Kozo Hori

Noriyuki Okujo

Keisuke Tohdo

Process for producing a 7-bromoquinolone-carboxylic acid derivative of the following formula or its salt by reacting a 2,4-dibromo-3-hydroxybenzoic acid ester compound of the formulaR-to obtain a 3-alkoxy-2,4-dibromobenzoic acid ester, subjecting the 3-alkoxy-2,4-dibromobenzoic acid ester to elimination reaction of the carboxyl-protecting group to obtain a 3-alkoxy-2,4-dibromobenzoic acid, subjecting the 3-alkoxy-2,4-dibromobenzoic acid to ketoesterification reaction to obtain a 3-alkoxy-2,4-dibromobenyolacetic acid ester, reacting the 3-alkoxy-2,4-dibromobenzoylacetic acid ester with an orthoester or an acetal, then reacting the reaction product with a compound of the formula R&#x2014;NH or its salt to obtain a 2-(3-alkoxy-2,4-dibromobenzoyl)-3-substituted aminoacrylic acid ester and subjecting the 2-(3-alkoxy-2,4-dibromobenzoyl)-3-substituted aminoacrylic acid ester to ring-closing reaction, and products thereof.

Processes for producing 7-isoindoline-quinolonecarboxylic acid derivative and its intermediate, as well as salt of 7-isoindoline-quinolonecarboxylic acid derivative, its hydrate and composition comprising the same as active ingredient

An arylamidine derivative represented by a general formula described below or a salt thereof has an excellent antifungal action and high safety, and it is useful as an antifungal agent with good pharmacokinetics and pharmacodynamic properties wherein X represents an unsubstituted or substituted lower alkylene or alkenylene group; Grepresents an oxygen atom, a sulfur atom, or an imino group; Grepresents a carbon atom or a nitrogen atom; Rrepresents at least one group selected from the group consisting of a hydrogen atom, a halogen atom, and unsubstituted or substituted alkyl, cycloalkyl and alkoxy groups; Rrepresents an unprotected or protected or unsubstituted or substituted amidino group; and Rrepresents a substituted amino or substituted cyclic amino group, or the like.

Arylamidine derivative or salt thereof

PROCESSES FOR PRODUCING 7-ISOINDOLINE-QUINOLONECARBOXYLIC ACID DERIVATIVE AND ITS INTERMEDIATE, AS WELL AS SALT OF 7-ISOINDOLINE-QUINOLONECARBOXYLIC ACID DERIVATIVE, ITS HYDRATE AND COMPOSITION COMPRISING THE SAME AS ACTIVE INGREDIENT

Processes for producing 7-isoindolinequinolonecarboxylic derivatives and intermediates therefor, salts of 7-isoindolinequinolonecarboxylic acids, hydrates thereof, and composition containing the same as active ingredient

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Toyama, Japan

Katsuji Ojima