反应详情

1.2 g of ethyl 1-[4-(tert-butoxycarbonylamino)-3-(2-isoindolin-2-yl-2-oxoacetyl)phenyl]cyclobutanecarboxylate are dissolved in 50 ml of acetonitrile under argon. 370 mg of caesium fluoride and 679 μl of bis(trimethylsilyl)carbodiimide are added to the solution. The mixture is stirred at room temperature for 15 min, and 6 ml of hydrochloric acid (1N) are then added, and the mixture is neutralised using bicarbonate. The aqueous phase is washed 3 times with 100 ml of ethyl acetate each time. The combined organic phases are dried over sodium sulfate, filtered and evaporated to dryness in vacuo. Yield: 1 g (99%) of ethyl 1-[2-amino-4-(isoindoline-2-carbonyl)quinazolin-6-yl]cyclobutanecarboxylate (oil);

1. washThe aqueous phase is washed 3 times with 100 ml of ethyl acetate each time
2. dry with materialThe combined organic phases are dried over sodium sulfate
3. filtrationfiltered
4. customevaporated to dryness in vacuo