反应详情

Using similar reaction conditions as described in step-i of example-1, tert-butyl 4-(5-(3-iodo-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyridin-2-yl)piperazine-1-carboxylate (Intermediate 66K) (200 mg, 0.303 mmol) was coupled with 1-(3-fluorobenzyl)-3-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (intermediate 12) (116 mg, 0.363 mmol) using sodium carbonate (96 mg, 0.909 mmol) and Pd(dppf)Cl2 (11 mg, 0.015 mmol) in toluene/ethanol/water (10/10/1 mL) to afford 250 mg (crude) of the titled compound after purification by column (Silica gel 60/120) using 50% ethyl acetate in hexane as eluent. MS: m/z=722.5 (M+1).

1. customreaction conditions