CRYSTALLINE FORM OF ANDROGEN RECEPTOR INHIBITOR AND PREPARATION METHOD THEREOF

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...

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Bibliographic Details
Main Authors WU, GUAILI, ZHONG, LIANG, LU, YUN, GUO, CHANGSHAN
Format Patent
LanguageEnglish
Polish
Published 21.09.2020
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary: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.
Bibliography:Application Number: PL20160843560T