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一種雄性激素受體抑制劑的結晶形式及其製備方法
专利权人:
JIANGSU HENGRUI MEDICINE CO.; LTD.
发明人:
WU, GUAILI,武乖利,GUO, CHANGSHAN,郭昌山,ZHONG, LIANG,锺良,鍾良,LU, YUN,卢韵,盧韵
申请号:
TW105128891
公开号:
TW201713628A
申请日:
2016.09.07
申请国别(地区):
TW
年份:
2017
代理人:
摘要:
The present invention relates a crystalline form of androgen receptor inhibitor and a preparation method thereof. In particular, the present invention relates a type I crystal of (S)-4-(3-(4-(2,3-dihydroxypropoxy)phenyl)-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile(formula I) and a preparation method thereof. The preparation method comprises 1) heating any crystal form or amorphous compound of formula (I) in a sufficient quantity organic solvent to obtain a solution, then cooling the solution to cause crystallization; said organic solvent is one or more of a solvent selected from the group consisting of ethyl acetate with no more than five carbons, acetone, nitrile, ether; 2) filtering, washing, and drying the crystals obtained in step 1). The type II crystal of compound of formula (I) obtained by the present invention has a good chemical stability and crystal stability, and the used crystal-solvent has a low toxicity and residue, which can be better used in clinical treatment.本發明涉及一種雄性激素受體抑制劑的結晶形式及其製備方法。具體地,本發明涉及(S)-4-(3-(4-(2,3-二羥基丙氧基)苯基)-4,4-二甲基-5-羰基-2-硫酮基咪唑啉-1-基)-2-(三氟甲基)苯甲腈(式(I)化合物)的I型結晶及其製備方法,所述方法包括:1)將任意晶型或無定型的式(I)所示化合物加入適量的有機溶劑中,加熱溶清後冷卻析晶,上述有機溶劑選自碳原子數小於等於5的酯類、酮類、腈類、醚類的任意一種或它們的混合溶劑;2)過濾結晶並洗滌,乾燥。本發明所得到式(I)化合物的I型結晶具備良好的化學穩定性和晶型穩定性,並且所用結晶溶劑低毒低殘留,可更好地用於臨床治療。
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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