反应详情

Using similar reaction conditions as described in step-i of example-1, tert-butyl 4-((3-(3-iodo-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)amino)piperidine-1-carboxylate (intermediate 66E) (200 mg, 0.297 mmol) was coupled with 1-phenethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (intermediate 59) (133 mg, 0.446 mmol) using Pd(PPh3)2Cl2 (11 mg, 0.014 mmol) and sodium carbonate (79 mg, 0.744 mmol) in toluene/ethanol/water (5/2/1 ml) to afford 150 mg (70.4% yield) of the titled compound after column purification using 1% methanol in DCM as eluent. MS: m/z=717.3 (M+1).

1. customreaction conditions