FIELD: medicine; pharmaceuticals.
SUBSTANCE: present invention relates to an improved method of producing 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-pyrazol-3-carboxamide (1A), and their key intermediate compounds, such as 2-chloro-4-(1H-pyrazol-3-yl) benzonitrile (V).
EFFECT: antagonists of AR are useful in treating cancer, particularly prostate cancer, and other diseases in which AR-antagonism is desirable.
22 cl, 7 ex
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Authors
Dates
2020-04-21—Published
2016-04-08—Filed