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    • 3. 发明申请
    • CRYSTALLINE FORMS OF 11 ß-(4-ACETYLPHENYL)-20,20,21,21,21-PENTAFLUOR-17- HYDROXY-19-NOR-17a-PREGNA-4,9-DIEN-3-ONE
    • 11 SS(4-乙酰基苯基)-20,20,21,21,的结晶形式21五氟-17-羟基-19-去-17A - 孕-4,9-二烯-3-酮
    • WO2007140917A3
    • 2008-04-10
    • PCT/EP2007004805
    • 2007-05-31
    • BAYER SCHERING PHARMA AGBECKMANN WOLFGANGWINTER GABRIELEKRAEMER EDDAGINKO THOMASAMOULONG EVELINCLEVE ARWED
    • BECKMANN WOLFGANGWINTER GABRIELEKRAEMER EDDAGINKO THOMASAMOULONG EVELINCLEVE ARWED
    • C07J1/00A61K31/567A61P5/36
    • C07J1/0081
    • The present invention relates to crystalline forms of 11 ß-(4-acetylphenyl)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17a-pregna-4,9-dien-3-one. In particular, the invention relates to two crystalline ansolvate/anhydrate forms of this compound, polymorphs I and II. However, the present invention also relates to crystalline solvates, for example, methanol and ethanol solvates of 11 ß-(4-acetylphenyl)- 20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17a-pregna-4,9-dien-3-one, as precursors for the preparation of these two polymorphs I and II. Processes are described for the preparation of polymorph I by means of displacement crystallization or by means of extraction. The choice of the last solvent, before the ansolvate formation can take place, on the basis of the differences in the purification ratios of the individual solvates of 11 ß-(4-acetylphenyl)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17a-pregna-4,9-dien-3-one is described. Polymorph I, according to the invention, is particularly suitable for the preparation of drugs.
    • 本发明涉及11 SS(4-乙酰苯基)的结晶形式 - 20,20,21,21,21五氟-17-羟基-19-去-17A - 孕-4,9-二烯-3-酮。 特别地,本发明涉及该化合物的两种结晶Ansolvat- / Anhydratformen,多晶型I和II,然而,本发明也涉及结晶溶剂化物,例如甲醇和β-11(4-乙酰基苯基)乙醇溶剂化物 - 20,20,21, 21,21五氟-17-羟基-19-去-17A - 孕-4,9-二烯-3-酮,为生产这些两种多晶型我的前体和II。有用于通过位移制备多晶型I或通过结晶方法 搅拌说明。 最终溶剂的Ansolvatbildung之前选择可在11 SS(4-乙酰苯基)-20,20,21,21,21五氟-17-羟基-19-去-17A - 孕的单独溶剂化物的纯化行为差异的基础上 -4,9-二烯-3-酮完成。 我根据本发明多晶型物是特别适合于生产药物。