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首页> 外文期刊>Crystal growth & design >Crystal Forms of Enzalutamide and a Crystal Engineering Route to Drug Purification
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Crystal Forms of Enzalutamide and a Crystal Engineering Route to Drug Purification

机译：烯醇酰胺的水晶形式和药物净化的晶体工程途径

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摘要

The crystal forms of the active pharmaceutical ingredient enzalutamide, a drug used for the treatment of metastatic prostate cancer, have been investigated by X-ray, thermogravimetric analysis, and differential scanning calorimetry techniques. The single crystal structure of the anhydrous form RI (marketed by Astellas) has been determined and compared with the powder diffraction data. Upon crystallization from Me0H and formic acid, a new solvate form called R2 has been discovered and characterized. The crystal structure of R2 contains voids that can host other small molecules such as formic acid, methanol, or water. Form R2 loses solvent at ca. 120-140 degrees C and recrystallizes into the stable unsolvated form R1. In the case of isopropyl alcohol, a solvate form R3 has also been obtained. R1 converts into R3 under slurry conditions in isopropyl alcohol. The structure of R3 has been determined from powder diffraction data. Importantly, while form R1 is easily contaminated with O-enzalutamide (the substitution impurity of S-enzalutamide) by forming stable solid solutions up to 50%, form R3 does not and can be used to easily purify the raw S-enzalutamide.
机译：通过X射线，热重分析和差示扫描量热法研究，研究了活性药物成分烯醇酰胺的晶体形式，用于治疗转移性前列腺癌的药物。已经确定并与粉末衍射数据确定了无水形式Ri（astellas销售）的单晶结构。在MEOH和甲酸中结晶后，已经发现并表征了一种称为R 2的新溶剂化物形式。 R2的晶体结构含有空隙，其可以托管其他小分子，例如甲酸，甲醇或水。形式R2在CA输掉溶剂。 120-140℃并将其重结晶到稳定的未经溶剂形式R1中。在异丙醇的情况下，还获得了溶剂化物形式R 3。 R1在异丙醇中的浆料条件下转化为R3。 R3的结构已经由粉末衍射数据确定。重要的是，通过形成稳定的固溶体易于形成高达50％的固体溶液容易被O-键胺（S-eNα-丁酰胺的取代杂质）容易被污染，而形式R3不且可用于容易净化未加工的S-苯甲酸丁酰胺。

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