首页> 外国专利> CRYSTALLINE FORMS OF 11 ß-(4-ACETYLPHENYL)-20,20,21,21,21-PENTAFLUOR-17- HYDROXY-19-NOR-17α-PREGNA-4,9-DIEN-3-ONE

CRYSTALLINE FORMS OF 11 ß-(4-ACETYLPHENYL)-20,20,21,21,21-PENTAFLUOR-17- HYDROXY-19-NOR-17α-PREGNA-4,9-DIEN-3-ONE

机译:11ß-(4-乙酰苯)-20,20,21,21,21-五元共聚物17-HYDROXY-19-NOR-17α-PREGNA-4,9-DIEN-3-ONE的晶体形式

摘要

The present invention relates to crystalline forms of 11 β - (4-acetylphenyl) -20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17α -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 β - (4-acetylphenyl) -20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17α-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 β - (4, acetylphenyl) -20,20,21,21,21-pentafluor -17-hydroxy-19-nor-17 α -pregna-4,9-dien-3-one is described. Polymorph I, according to the invention, is particularly suitable for the preparation of drugs.
机译:本发明涉及11β-(4-乙酰基苯基)-20,20,21,21,21-五氟-17-羟基-19-nor-17α-pregna-4,9-dien-3-one的结晶形式。特别地,本发明涉及该化合物的两种结晶无溶剂化物/无水形式,多晶型物I和II。然而,本发明还涉及结晶溶剂化物,例如11β-(4-乙酰基苯基)-20,20,21,21,21-五氟-17-羟基-19-nor-17α-的甲醇和乙醇溶剂化物。 pregna-4,9-dien-3,一种,作为制备这两种多晶型物I和II的前体。描述了通过置换结晶或通过萃取制备多晶型物I的方法。根据11β-(4,乙酰苯基)-20,20,21,21,21-五氟的各个溶剂化物的纯化比率的差异,在形成溶剂化物之前选择最后一种溶剂描述了-17-羟基-19-nor-17α-pregna-4,9-dien-3-one。根据本发明的多晶型物I特别适合于制备药物。

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