反应详情

To a solution of tert-butyl 4-[(2E)-4-{4-[(3-chloro-4-fluorophenyl)amino]-5,8-dihydropyrido-[4′,3′:4,5]thieno[2,3-d]pyrimidin-7(6H)-yl}-4-oxobut-2-en-1-yl]piperazine-1-carboxylate from Example 3 (150 mg, 0.255 mmol) in dichloromethane (15 mL) was added TFA (1.0 mL, 13 mmol), and the mixture was stirred at rt for 5 h. The solvent was removed in vacuo. 1 M aqueous sodium hydroxide solution was added, and the mixture was extracted with ethyl acetate. The organic layer was dried over sodium sulfate, and the solvent was evaporated. The residue was crystallized from dichloromethane/diethyl ether to yield 108 mg (87%) of the title compound.

1. customThe solvent was removed in vacuo
2. addition1 M aqueous sodium hydroxide solution was added
3. extractionthe mixture was extracted with ethyl acetate
4. dry with materialThe organic layer was dried over sodium sulfate
5. customthe solvent was evaporated
6. customThe residue was crystallized from dichloromethane/diethyl ether