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) (150 mg, 0.227 mmol) was coupled with 1-phenethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (Intermediate 59) (101 mg, 0.34 mmol) using sodium carbonate (73 mg, 0.68 mmol) and Pd(PPh3)2Cl2 (10 mg, 0.011 mmol) in toluene/ethanol/water (3/5/1 ml) to afford 140 mg (88.0% yield) of the pure product after column purification using 5% methanol in dichloromethane as eluent. MS: m/z=704.3 (M+1).

1. customreaction conditions