反应详情

A similar procedure as described in Example 40, step 7 was used, starting from 4-{2-(2-ethoxycarbonyl-ethyl)-3-[6-(3-iodo-5-methanesulfonyl-phenoxy)-hexyl]-phenoxy}-butyric acid ethyl ester (150 mg, 0.22 mmol), 1H-pyrazol-3-ylboronic acid (51.4 mg, 0.45 mmol), tetrakis(triphenylphosphine)palladium(0) (50.8 mg, 0.04 mmol), and potassium carbonate (30.2 mg, 0.22 mmol) to afford 4-(2-(2-ethoxycarbonyl-ethyl)-3-{6-[3-methanesulfonyl-5-(1H-pyrazol-3-yl)-phenoxy]-hexyl}-phenoxy)-butyric acid ethyl ester (39 mg, 28.5%) as a light brown viscous oil: ES(+)-HRMS m/e calcd for C33H44N2O8S (M+H)+ 629.2891, found 629.2894.