反应详情

A mixture of 4-[(phenylmethyl)oxy]-1H-indazole (D1) (530 mg, 2.37 mmol), {3-fluoro-4-[(phenylmethyl)oxy]phenyl}boronic acid (873 mg, 3.55 mmol), copper acetate (861 mg, 4.74 mmol), triethylamine (0.660 mL, 4.74 mmol) and powdered 4A molecular sieves (2.5 g) in dichloromethane (10 mL) was stirred vigorously under an air atmosphere at ambient temperature. Further quantities of boronic acid, triethylamine and copper acetate were added after 18 hours (0.5 equivalents of each) and 22 hours (1 equivalent of each). After stirring for a further 24 hrs, the mixture was filtered through a plug of silica gel and concentrated. Chromatography (silica gel, elution with 0-20% ethyl acetate in hexane) gave the title compound (D2) as a white solid (309 mg).

1. stirringAfter stirring for a further 24 hrs
2. filtrationthe mixture was filtered through a plug of silica gel
3. concentrationconcentrated
4. washChromatography (silica gel, elution with 0-20% ethyl acetate in hexane)