反应详情

(5-Bromo-2-methoxy-phenyl)-[4-(2,4-difluoro-phenylamino)-phenyl]-methanone (1.00 g; 2.37 mmol), 4-prop-2-ynyl-morpholine (1.2 g; 9.5 mmol) PdCl2(PPh3)2 (320 mg; 0.4 mmol), Cs2CO3 (2.0 g; 6.2 mmol) and CuI (100 mg; 0.52 mmol) are dissolved in diethylene glycol dimethyl ether (10 ml) and N,N-diisopropylethylamine (5 ml) and heated to 140° C. for 1 hour. The reaction mixture is diluted with TBME, filtered, evaporated and purified by chromatography (SiO2, acetone/hexanes 3/7>6/4) to yield the title compound as yellow foam (445 mg; 40%).

1. filtrationfiltered
2. customevaporated
3. custompurified by chromatography (SiO2, acetone/hexanes 3/7>6/4)