反应详情

温度

70 °C

200 mg (0.52 mmol) of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]-7-bromo-1-benzofuran-2-carboxamide hydrochloride (Example 30A) and 106.8 mg (0.52 mmol) of 3-(trifluoromethoxy)phenylboronic acid are introduced into 2.0 ml of DMF. Addition of 0.78 ml of 2 M sodium carbonate solution and 21.2 mg (0.03 mmol) of PdCl2(dppf) is followed by heating at 70° C. for 17 h. After cooling, the reaction mixture is filtered through kieselguhr and purified by preparative HPLC. The product fractions are combined and concentrated and, after addition of a 5:1 mixture of methanol and 1N hydrochloric acid, again concentrated. Drying under high vacuum results in 48.8 mg (20% of theory) of the title compound.

1. temperatureAfter cooling
2. filtrationthe reaction mixture is filtered through kieselguhr
3. custompurified by preparative HPLC
4. concentrationconcentrated
5. additionafter addition of a 5:1 mixture of methanol and 1N hydrochloric acid
6. concentrationagain concentrated
7. customDrying under high vacuum