反应详情

Using similar reaction conditions as described in step-ii of intermediate 1, tert-butyl 4-(4-(3-iodo-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperazine-1-carboxylate (intermediate 41) (400 mg, 0.6 mmol) was coupled with 3,5-dimethyl-1-(3-nitrobenzyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (intermediate 56) (240 mg, 0.66 mmol) in sodium carbonate (196 mg, 1 mmol), PdCl2(dppf) (22 mg, 0.03 mmol), toluene/ethanol/water (2/2/2 ml) to give 200 mg (43% yield) of titled compound after purification by column (SiO2) using 30% ethyl acetate in hexane as eluent. MS: m/z=762.3 (M+1).

1. customreaction conditions