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-methoxyphenyl)piperidine-1-carboxylate (intermediate 67A) (260 mg, 0.378 mmol) was coupled with 1-(3-fluorobenzyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (intermediate 11) (172 mg, 0.567 mmol) using Pd(dppf)Cl2 (14 mg, 0.018 mol) and sodium carbonate (121 mg, 1.134 mmol) in toluene/ethanol/water (6/2/1 ml) to afford 200 mg (71.9% yield) of the titled compound after column purification using 2% methanol in DCM as eluent. MS: m/z=736.4 (M+1).

1. customreaction conditions