Synthesis Process of Darolutamide Intermediate 2-Chloro-4-(1H-pyrazole-3-yl)benzonitrile
2-Chloro-4-(1H-pyrazole-3-yl)benzonitrile is an important intermediate fragment of the no-vel anti-prostate cancer drug darolutamide.In this paper,4-bromo-2-chlorobenzonitrile and 1-(tetra-hydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole were chosen as the raw materials.Through Suzuki coupling and hydrolysis deprotection reactions,2-chloro-4-(1H-pyrazole-3-yl)benzonitrile was obtained with a total yield of over 95％and a purity of over 99％at the reaction scale of 50 g.The reaction has several advantages of safe and easy available raw materials,simple separation of the product,high yield and high product purity,especially the mother liquor of the Suzuki coupling reaction in the first step can be recycled,saving Pd catalyst and production costs,which are all suitable for industrial production.
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