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Crystalline form of a male hormone receptor inhibitor and its preparation method

机译:雄性激素受体抑制剂的晶型及其制备方法

摘要

A crystalline form of an androgen receptor inhibitor is provided and a method of preparation thereof. in particular, type I crystal of (4-) (3- (4- (2,3-dihydroxypropoxy) phenyl) -4,4-dimethyl-5-carbonyl-2-thioimidazolin-1 is provided. -yl) -2- (trifluoromethyl) benzonitrile (a compound of formula (i)) and a method of preparation thereof, wherein the method comprises: 1) any crystalline or amorphous form of the compound as shown by formula (i) It is added to an appropriate amount of an organic solvent, heated and dissolved until clear, thereafter cooled and crystallized, wherein the organic solvent is selected from any of esters, ketones, nitriles and ethers having 5 or fewer carbon atoms, or a mixed solvent thereof; and 2) the crystal is filtered, washed and dried. The type I crystal obtained from the compound of formula (I) has good chemical stability and crystalline stability, and the crystallization solvent used has low toxicity and residue, and may be better used for clinical treatment.
机译:提供了一种雄激素受体抑制剂的结晶形式及其制备方法。特别地,提供(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的I型晶体。-yl)-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)如式(i)所示的化合物的任何结晶或无定形形式将其添加至适当的量将有机溶剂加热并溶解直至澄清,然后冷却并结晶,其中有机溶剂选自具有5个或更少碳原子的酯,酮,腈和醚中的任何一种,或其混合溶剂; 2)将晶体过滤,洗涤并干燥。由式(I)的化合物获得的I型晶体具有良好的化学稳定性和晶体稳定性,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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