发明名称 CRYSTAL OF N-[2-({2-[(2S)-2-CYANOPYRROLIDIN-1-YL]-2- OXOETHYL}AMINO)-2-METHYLPROPYL]-2-METHYLPYRAZOLO[1,5-a]PYRIMIDINE-6-CARBOXAMIDE
摘要 <p>[Problem] To provide: a crystal of anagliptin, which has high purity, excellent stability, low hygroscopicity and a property of being dissolved in water extremely satisfactorily; and a method for producing the crystal of anagliptin. [Solution] A crystal of anagliptin, which has peaks at points located adjacent to diffraction angles, each of which is expressed in 2theta, of 9.8°, 17.4°, 18.6°, 25.3° and 25.8° and has substantially the same powder X-ray diffraction pattern as that illustrated in fig. 1. The crystal can be produced by reacting N-(2-amino-2-methylpropyl)-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide with (2S)-N-chloroacetyl- 2-cyanopyrrolidine in an organic solvent, then purifying the resultant product by column chromatography to produce an amorphous form of anagliptin, and then crystallizing the amorphous form of anagliptin from 2-propanol.</p>
申请公布号 WO2014034626(A1) 申请公布日期 2014.03.06
申请号 WO2013JP72793 申请日期 2013.08.27
申请人 SANWA KAGAKU KENKYUSHO CO., LTD. 发明人 SAKAIRI MASAO;INAGAKI HIDEAKI;OKA MITSURU;MURASE TAKAYO
分类号 C07D487/04;A61K31/519;A61P3/10 主分类号 C07D487/04
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