Generated: April 23, 2017
|Title:||.alpha.-form or .beta.-form crystal of acetanilide derivative|
|Abstract:||To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with .alpha.-form crystal and .beta.-form crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenyleth-yl)amino]ethyl]- acetanilide. The .alpha.-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The .beta.-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the .alpha.-form crystal.|
|Inventor(s):||Kawazoe; Souichirou (Takahagi, JP), Sakamoto; Kenichirou (Takahagi, JP), Awamura; Yuji (Tsukuba, JP), Maruyama; Tatsuya (Tsukuba, JP), Suzuki; Takayuki (Tsukuba, JP), Onda; Kenichi (Tsukuba, JP), Takasu; Toshiyuki (Tsukuba, JP)|
|Assignee:||Astellas Pharma Inc. (Tokyo, JP)|
1. A crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]a- cetanilide having a heat absorption peak at 142 to 146.degree. C. in the DSC
analysis and having main peaks at around 5.32, 8.08, 15.28, 17.88, 9.04, 20.20, 23.16 and 24.34 in the terms of 2.theta.(.degree.) in the powder X-ray diffraction.
2. A crystal of (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]a- cetanilide having heat absorption peaks at 90 to 110.degree. C. and at 142 to 146.degree. C. in the DSC analysis and having main peaks at around 9.68, 19.76, 20.72, 22.10 and 23.52 in the terms of 2.theta.(.degree.) in the powder X-ray diffraction.
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