1-(hydroxymethyl)cyclopropanesulfonamide 、 2-[4-(difluoromethylidene)piperidin-1-yl]-N-[2-(4,4-difluoropiperidin-1-yl)-6-methylpyrimidin-4-yl]-4-iodobenzamide 在
potassium phosphate 、
copper(l) iodide 、
肌氨酸 作用下,
以
N,N-二甲基甲酰胺 为溶剂,
以32 %的产率得到2-[4-(difluoromethylidene)piperidin-1-yl]-N-[2-(4,4-difluoropiperidin-1-yl)-6-methylpyrimidin-4-yl]-4-[[1-(hydroxymethyl)cyclopropyl]sulfonylamino]benzamide