反应详情

3 ml of triethylamine, 368.7 μl of 2-propyn-1-ol, 36.6 mg of copper(I) iodide and 67.5 mg of bis(triphenylphosphine)palladium(II) chloride (15.2% of palladium) are added to a solution of 2 g of 2-amino-6-iodo-4-(1,3-dihydroisoindol-2-ylcarbonyl)quinazoline in 3 ml of DMF under argon. The mixture is stirred at room temperature for 48 h, 100 ml of DCM are added, and the mixture is subjected to aqueous extraction a number of times. The organic phase was dried and evaporated to dryness under reduced pressure in a rotary evaporator. A little ACN is added to the residue obtained, during which a yellow solid precipitates out. Filtration and drying (drying cabinet at 40° C.) gives 1.3 g of “A964”;

1. extractionthe mixture is subjected to aqueous extraction a number of times
2. customThe organic phase was dried
3. customevaporated to dryness under reduced pressure in a rotary evaporator
4. additionA little ACN is added to the residue
5. customobtained, during which a yellow solid
6. customprecipitates out
7. filtrationFiltration
8. customdrying
9. custom(drying cabinet at 40° C.)
10. customgives 1.3 g of “A964”