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CRYSTALLINE FORM OF ANDROGEN RECEPTOR INHIBITOR AND PREPARATION METHOD THEREOF

机译:雄激素受体抑制剂的晶体形式及其制备方法

摘要

Provided are a crystalline form of an androgen receptor inhibitor and a preparation method thereof. In particular, provided are type I crystal of (S)-4-(3-(4-(2,3-dihydroxypropoxy)phenyl)-4,4-dimethyl-5-carbonyl-2-thioimidazolin-1-yl)-2-(trifluoromethyl)benzonitrile (a compound of formula (I)) and a preparation method thereof, wherein the method comprises: 1) any crystal form or amorphous form of the compound as shown by formula (I) is added to an appropriate amount of an organic solvent, heated and dissolved until clear, following by being cooled down and crystallized, wherein the organic solvent is selected from any one of esters, ketones, nitriles and ethers which have 5 or less carbon atoms, or a mixed solvent thereof; and 2) the crystal is filtered, washed and dried. The obtained type I crystal of the compound of formula (I) has a good chemical stability and crystal form stability, and the crystallization solvent used has a low toxicity and residue, and can be better used for clinical treatment.
机译:提供了一种雄激素受体抑制剂的晶型及其制备方法。特别地,提供了(S)-4-(3-(4-(2,3-二羟基丙氧基)苯基)-4,4-二甲基-5-羰基-2-硫代咪唑啉-1-基)-的I型晶体。 2-(三氟甲基)苄腈(式(I)的化合物)及其制备方法,其中该方法包括:1)以适当的量加入式(I)所示化合物的任何晶形或无定形形式加热并溶解直至澄清的有机溶剂,然后冷却并结晶,其中所述有机溶剂选自具有5个以下碳原子的酯,酮,腈和醚中的任何一种,或它们的混合溶剂; 2)将晶体过滤,洗涤并干燥。所获得的式(I)化合物的I型晶体具有良好的化学稳定性和晶形稳定性,并且所使用的结晶溶剂具有低毒性和残留物,并且可以更好地用于临床治疗。

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