Process for the preparation of (-)-1,4-benzothiazine-2-acetic acid derivatives

A process for the preparation of (-)-1,4-benzothiazine-2-acetic acid derivatives, characterized by conducting the optical resolution of a racemic modification of a 1,4-benzothiazine-2-acetic acid derivative represented by general formula (I) by forming a salt of the (-)-enantiomer of the derivative...

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Hauptverfasser: YUJI ONO, TSUGUO IKEBE, SATORU UEMORI, FUMIHIKO AKAHOSHI, AKIHIKO MORIGUCHI
Format: Patent
Sprache:eng
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Zusammenfassung:A process for the preparation of (-)-1,4-benzothiazine-2-acetic acid derivatives, characterized by conducting the optical resolution of a racemic modification of a 1,4-benzothiazine-2-acetic acid derivative represented by general formula (I) by forming a salt of the (-)-enantiomer of the derivative with an optically active substance: (wherein R and R are each hydrogen or the like; R is carboxyl or the like; R , R , R and R are each hydrogen, halogeno, or the like; and X is oxygen or the like). This process makes it possible to separate (-)-1,4-benzothiazine-2-acetic acid derivatives respectively from the corresponding (+/-)-1,4-benzothiazine-2-acetic acid derivatives in high yield and at high optical purity.