CRYSTAL OF N-[2-(AMINO)-2-METHYLPROPYL]-2-METHYLPYRAZOLO[1,5-A]PYRIMIDINE-6-CARBOXAMIDE

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United States of America Patent

APP PUB NO 20150239890A1
SERIAL NO

14423170

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Abstract

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An object is to provide a crystal of anagliptin, which has a high purity and is excellent in stability, low in hygroscopicity, and has a characteristic of easily dissolving into water, and a method for producing the crystal. An anagliptin crystal showing a powder X-ray diffraction pattern substantially the same as in FIG. 1, which has peaks around at 9.8°, 17.4°, 18.6°, 25.3°, and 25.8° as diffraction angles represented by 2θ. The crystal is obtained by reacting N-(2-amino-2-methylpropyl)-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide and (2S)—N-chloroacetyl-2-cyanopyrrolidine in an organic solvent, thereafter purifying the reaction solution by column chromatography to thus obtain an amorphia of anagliptin, and crystallizing the amorphia of anagliptin from 2-propanol.

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Patent Owner(s)

Patent OwnerAddress
SANWA KAGAKU KENKYUSHO CO LTD35 HIGASHISOTOBORI-CHO HIGASHI-KU NAGOYA-SHI AICHI 4618631 ?4618631

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Inagaki, Hideaki Mie, JP 8 32
Murase, Takayo Mie, JP 3 15
Oka, Mitsuru Mie, JP 8 29
Sakairi, Masao Mie, JP 4 15

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