反应详情

(4Z)-6-Bromo-4-{[(3-hydroxy-4-propoxybenzyl)amino]methylene}isoquinoline-1,3(2H,4H)-dione (110 mg, 0.255 mmol) is mixed with 3-furanboronic acid (58 mg, 0.51 mmol), Pd2(dba)3 (35 mg, 0.038 mmol), and cesium carbonate (166 mg, 0.51 mmol). After the solids were degassed, N,N-dimethylformamide (1.7 mL) and P(t-Bu)3 (15.5 mg, 0.077 mmol) were added. The mixture is heated at 100 C for 1 h, diluted with methylene chloride, and filtered. The filtrate is evaporated to dryness and purified by column chromatography to yield 8.5 mg (8%) of the title compound as a white solid. MS (ESI) m/z 417, 419 (M+H)+1

1. customAfter the solids were degassed
2. temperatureThe mixture is heated at 100 C for 1 h
3. filtrationfiltered
4. customThe filtrate is evaporated to dryness
5. custompurified by column chromatography