反应详情

(4Z)-6-Iodo-4-({[2-(4-methylpiperazin-1-yl)pyrimidin-5-yl]amino}methylene)isoquinoline-1,3(2H,4H)-dione (73.5 mg, 0.15 mmol) is mixed with 3-furanboronic acid (33 mg, 0.3 mmol), Pd2(dba)3 (20.6 mg, 0.022 mmol), and cesium carbonate (98 mg, 0.3 mmol). After the solids were degassed, N,N-dimethylformamide (1.05 mL) and P(t-Bu)3 (9.1 mg, 0.045 mmol) were added. The mixture is heated at 100 C for 55 min, diluted with methylene chloride, and filtered. The filtrate is evaporated to dryness and purified by column chromatography to yield 36 mg (55%) of the title compound as a yellow solid. MS (ESI) m/z 431 (M+H)+1

1. customAfter the solids were degassed
2. temperatureThe mixture is heated at 100 C for 55 min
3. filtrationfiltered
4. customThe filtrate is evaporated to dryness
5. custompurified by column chromatography