反应详情

Using similar reaction conditions as described in step-i of example-1, tert-butyl 4-(5-(3-iodo-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyridin-2-yl)piperazine-1-carboxylate (Intermediate 66K) (300 mg, 0.454 mmol) was coupled with 1-(3-(benzyloxy)benzyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (intermediate 64E) (195 mg, 0.500 mmol) using sodium carbonate (145 mg, 1.364 mmol) and Pd(dppf)Cl2 (17 mg, 0.022 mmol) in toluene/ethanol/water (3/3/2 mL) to afford 250 mg (69% yield) of the titled compound after purification by column (Silica gel 60/120) using 0.5% methanol in DCM as eluent. MS: m/z=796.3 (M+1).

1. customreaction conditions