反应详情

Using similar reaction conditions as described in step-i of example-1, tert-butyl 4-(2-fluoro-4-(3-iodo-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate (intermediate 66Q) (300 mg, 0.445 mmol) was coupled with 1-(3-fluorobenzyl)-3,5-dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (intermediate 16) (177 mg, 0.534 mmol) using Pd(dppf)Cl2 (16 mg, 0.022 mol) and sodium carbonate (141 mg, 1.335 mmol) in toluene/ethanol/water (5/8/1 mL) to afford 250 mg (74.8% yield) of the titled compound. MS: m/z=750.4 (M+1).

1. customreaction conditions