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)benzyl)piperidine-1-carboxylate (intermediate 66G) (300 mg, 0.44 mmol) was coupled with 1-(3-fluorobenzyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (intermediate 11) (170 mg, 0.58 mmol) using Pd(DPPF)Cl2 (15 mg, 0.02 mmol) and sodium carbonate (140 mg, 1.32 mmol) in toluene/ethanol/water (15/8/4 ml) to afford 200 mg (62.3% yield) of the titled compound after column purification using 30% ethyl acetate in hexane as eluent. MS: m/z=720.3 (M+1).

1. customreaction conditions