Kissei Pharmaceutical Co., Ltd.

Michio Toda

Kiyoshi Kasai

Eiji Tsuru

Nobuyuki Tanaka

Tetsuro Tamai

Hidetoshi Isawa

Junichi Sonehara

Kazuma Hirata

The present invention provides ethyl (&#x2212;)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride &#xbc; hydrate or a crystal thereof which can be determined by characteristic diffraction peaks of the powder X-ray diffraction, thermogravimetry-differential thermal analysis or the like, and obtained by manufacturing ethyl (&#x2212;)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methyl-ethyl]amino]ethyl]-2,5-dimethylphenoxyacetate by a specific method.

Crystal of hydroxynorephedrin derivative hydrochloride &#xbc; hydrate

The present invention provides a novel crystal polymorph of ethyl (&#x2212;)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride which can be determined by characteristic diffraction peaks of the powder X-ray diffraction or the like, and obtained from ethyl (&#x2212;)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate by a specific method.

Crystal polymorph of hydroxynorephedrin derivative hydrochloride

The present invention relates to a crystalline polymorph of 2-&lsqb;4-&lsqb;2-&lsqb;&lsqb;(1S,2R)-2-hydroxy-2-(4-hydroxy-phenyl)-1-methylethyl&rsqb;amino&rsqb;ethyl&rsqb;phenoxy&rsqb;acetic acid having strong diffraction peaks (diffraction angle: 2&thgr;&plusmn;0.1&deg;) at 10.8, 19.1, 19.3, 19.8, 20.6 and 27.0&deg; in powder X-ray diffraction pattern, which has potent &bgr; - and &bgr; -adrenoceptor stimulating effects and is useful as an agent for relieving pain and promoting the removal of calculi in urolithiasis, and the like. For example, the crystalline polymorph can be prepared by hydrolyzing ethyl 2-&lsqb;4-&lsqb;2-&lsqb;&lsqb;(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl&rsqb;-amino&rsqb;ethyl&rsqb;phenoxy&rsqb;acetate phosphate by sodium hydroxide, adding an aqueous phosphoric acid solution at 40&deg; C. and over, adding a mixed solvent of water and methanol or methanol to the resulting compound, and stirring the suspension at 40&deg; C. to reflux temperature for 30 minutes to several hours.

Crystal polymorphism of aminoethylphenoxyacetic acid derivative

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Matsumoto, Japan

Michio Toda