Toyama Chemical Co., Ltd.

Naokatu Aoki

Tamotsu Takamatsu

Kenji Yonezawa

Tomohiro Hashimoto

Junichi Mitsuyama

Yoshiaki Suzuki

Masahiro Takebayashi

Yuji Oonishi

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

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Toyama, Japan

Naokatu Aoki