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)-2-nitrophenyl)piperazine-1-carboxylate (intermediate 66J) (340 mg, 0.48 mmol) was coupled with 1-(3-fluorobenzyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (intermediate 11) (189 mg, 0.628 mmol) using Pd(dppf)Cl2 (18 mg, 0.024 mol) and sodium carbonate (152 mg, 1.44 mmol) in toluene/ethanol/water (20/10/5 ml) to afford 120 mg (33.05% yield) of the titled. MS: m/z=752.2 (M+1).

1. customreaction conditions
2. customto afford 120 mg (33.05% yield) of the