反应详情

Using similar reaction conditions as described in step-i of example-1, tert-butyl 4-(4-(3-iodo-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperidine-1-carboxylate (intermediate 67B) (200 mg, 0.304 mmol) was coupled with 3-((4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)methyl)pyridine (intermediate 64) (104 mg, 0.364 mmol) using Pd(dppf)Cl2 (11 mg, 0.015 mol) and sodium carbonate (97 mg, 0.912 mmol) in acetonitrile/water (3/1 ml) to afford 150 mg (72.0% yield) of the titled compound after column purification using 3% methanol in DCM as eluent.

1. customreaction conditions