反应详情

(5-(4-[3-Chloro-4-(3-fluoro-benzyloxy)-phenylamino]-quinazolin-6-yl)-furan-2-ylmethyl)-carbamic acid tert-butyl ester (0.0218 g, 0.0379 mmol) is dissolved in DCM (2 ml) and TFA (2 ml) is added dropwise. The reaction mixture is stirred at room temperature for 1 hour. The solvent is removed under a nitrogen stream and to the residue are added consecutively saturated aqueous potassium carbonate solution and DCM. The resulting mixture is extracted with DCM containing 5% THF, the combined organic extracts are dried (Na2SO4) and concentrated under reduced pressure to yield 17.6 mg (0.037 mmol, 98%) of the clean desired product.

1. customThe solvent is removed under a nitrogen stream
2. additionto the residue are added consecutively saturated aqueous potassium carbonate solution and DCM
3. extractionThe resulting mixture is extracted with DCM containing 5% THF
4. dry with materialthe combined organic extracts are dried (Na2SO4)
5. concentrationconcentrated under reduced pressure