反应详情

Using similar reaction conditions as described in step-i of example-1, 5-bromo-3-(1-phenethyl-1H-pyrazol-3-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridine (intermediate 63A) (160 mg, 0.307 mmol) was coupled with tert-butyl 4-(2-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate (intermediate 70) (307 mg, 0.769 mmol) using potassium phosphate (195 mg, 0.918 mmol), tricyclohexyl phosphine (13 mg, 0.046 mmol) and Pd2(dba)3 (28 mg, 0.030 mmol) in dioxane/water (15/3 ml) to afford 126 mg (57.2% yield) of the pure product after column purification using 35% ethyl acetate in hexane as eluent. MS: m/z=718.3 (M+1).

1. customreaction conditions