Toyama Chemical Co., Ltd.

Kenji Yonezawa

Tamotsu Takamatsu

Yoshiaki Suzuki

Hironori Kotsubo

Taro Kiyoto

Akihito Saitoh

Minako Yotsuji

Kazuya Hayashi

Tomohiro Hashimoto

Katsuji Ojima

Hirohiko Yamamoto

Kyoko Taya

Masahiro Takebayashi

Mitsuhide Kawamura

Takahiko Kusanagi

Takashi Nakai

Naokatu Aoki

Yuji Oonishi

Minoru Yamada

Shoichi Hamamoto

Hiroko Matsukura

Kazuko Takaoka

Yasutaka Baba

Yukie Tada

A Process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a starting compound as a (phenylthio)acetic acid derivative or salts thereof represented by the general formula: wherein Xrepresents a halogen atom,is useful as a safe process for mass production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which is useful as a remedy for disease of central and peripheral nerve.

Process for production of 1-(3-(2-(1-benzothiophen-5-yl)-ethoxy)propyl)azetidin-3-ol or salts thereof

Disclosed is an organic amine salt of 6-fluoro-3-hydroxy-2-pyrazinecarbonitrile, which is excellent in crystallinity and useful as a production intermediate for 6-fluoro-3-hydroxy-2-pyrazinecarboxamide.

Organic amine salt of 6-fluoro-3-hydroxy-2-pyrazinecarbonitrile and method for producing the same

A 6-(halomethyl)-1,2-benzisoxazol-3(2H)-one derivative represented by the formula: wherein Ris a methyl group that is substituted with one or more optionally substituted phenyl groups, or an optionally substituted oxygen-containing heterocyclic group; and X is a halogen atom.

Process for production of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-OXO-2-substituted-2,3-dihydro-1,2-benzisoxazol-6-yl)methoxy]phenyl]propionate ester and intermediate for the process

A preparation method using as an intermediate 6-(halomethyl)-1,2-benzisoxazol-3(2H)-one derivative represented by general formula wherein Ris a methyl group that is substituted with one or more optionally substituted phenyl groups, or an optionally substituted oxygen-containing heterocyclic group; X represents a halogen atom, can be used as a method for safely and easily preparing 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid, which is useful as an antirheumatic agent, with a high yield.

Process for production of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-OXO-2-substituted-2,3-dihydro-1,2-benzisoxazol-6-yl]methoxy]phenyl]proprionate ester and intermediate for the process

The crystal of 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid having peaks at the position of 14.0, 16.0, 23.3, 23.7 and 26.3&#xb0; and the crystal of 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid having peaks at the position of 14.6, 23.1, 24.7, 25.6 and 26.0&#xb0; on 2&#x3b8; of diffraction angle in a powder X-ray diffraction pattern have a small specific volume, are hard to be charged with electricity, are easily handled and are useful for an active pharmaceutical ingredient of excellent anti-rheumatic agents.

Crystal of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl]propionic acid

A Process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a starting compound as a (phenylthio)acetic acid derivative or salts thereof represented by the general formula: wherein Xrepresents a halogen atom, is useful as a safe process for mass production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which is useful as a remedy for disease of central and peripheral nerve.

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

Kenji Yonezawa