反应详情

A mixture 4-(trifluoromethyl)phenylboronic acid (987 mgs, 5.2 mmol), 7-Bromo-3,4-dihydro-1H-isoquinoline-2-carboxylic acid tert-butyl ester (1.2 g, 4.0 mmol), potassium carbonate (1.1 g, 8.0 mmol), PdCl2(dppf) (146 mgs, 0.2 mmol) in toluene/ethanol/water (3 mL/1.5 mL/1.5 mL) was heated in pressure vessel at 120° C. for 2 h. The mixture was then concentrated and chromatographed (40 grams of SiO2, 30% EtOAc/hexanes) to provide the title compound (1.4 g, 92% yield over two steps).

1. concentrationThe mixture was then concentrated
2. customchromatographed (40 grams of SiO2, 30% EtOAc/hexanes)