PROCESS FOR THE PREPARATION OF ANDROGEN RECEPTOR ANTAGONISTS AND INTERMEDIATES THEREOF

PROCESS FOR THE PREPARATION OF ANDROGEN RECEPTOR ANTAGONISTS AND INTERMEDIATES THEREOF

The present invention relates to an improved process for the preparation of carboxamide structured androgen receptor (AR) antagonists such as N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H- pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3- carboxamide (1A) and key intermediates thereof such as 2...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: KARJALAINEN, OSKARI, LAITINEN, ILPO
Format: Patent
Sprache:eng ; fre
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:The present invention relates to an improved process for the preparation of carboxamide structured androgen receptor (AR) antagonists such as N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H- pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3- carboxamide (1A) and key intermediates thereof such as 2-chloro-4- (IH-pyrazol-3-yl)benzonitrile (V). AR antagonists are useful in the treatment of cancer, particularly prostate cancer and other diseases where AR antagonism is desired. La présente invention concerne un procédé amélioré de préparation d'antagonistes des récepteurs androgéniques (AR) structurés carboxamide tels que le N-((S)-1-(3-(3-chloro-4-cyanoph2nyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxy2thyl)-1H-pyrazole-3-carboxamide (1A) et de leurs intermédiaires clés tels que le 2-chloro-4-(1H-pyrazol-3-yl)benzonitrile (V). Les antagonistes AR sont utiles dans le traitement du cancer, particulièrement du cancer de la prostate et d'autres maladies dans lesquelles l'antagonisme AR est souhaité.