反应详情

(2-tert-Butoxycarbonylamino-thiazol-5-yl)-propynoic acid ethyl ester (1.2 g, 4.049 mmol) was dissolved in DCM (20 ml), trifluoroacetic acid (4.617 g, 40.93 mmol) was added in drop wise fashion at 0° C. After complete addition the reaction was allowed to stir for overnight at room temperature. Additional 3 ml of TFA was charged to the reaction and stirred for 2 hr. TLC showed complete reaction. Reaction was basified with sat. bicarbonate. The aqueous layer was extracted with ethyl acetate (30 ml×3). The combined organic layer was washed with water followed by brine and dried over anhydrous sodium sulfate and the solvent was removed on vacuo. The sticky solid product was obtained (0.700 g)

1. additionAfter complete addition the reaction
2. stirringstirred for 2 hr
3. customreaction
4. customReaction
5. extractionThe aqueous layer was extracted with ethyl acetate (30 ml×3)
6. washThe combined organic layer was washed with water
7. dry with materialdried over anhydrous sodium sulfate
8. customthe solvent was removed on vacuo
9. customThe sticky solid product was obtained (0.700 g)