反应详情

To a solution of 0.12 g (0.28 mMol) 4-fluoro-N-[4-methoxy-7-(1,2,3,6-tetrahydro-pyridin-4-yl)-benzothiazol-2-yl]-benzamide hydrochloride in 3 ml THF were added 0.043 ml triethyl amine. At 0° C. 0.029 ml (0.31 mMol) acetic anhydride was added dropwise and stirred for 30 min. Then a mixture of 5 ml sat. aqueous sodium bicarbonate and 15 ml water were added. After extracting with four times 25 ml ethyl acetate the combined organic phases were dried over sodium sulfate and concentrated to dryness in vacuo to yield 0.088 g (73%) N-[7-(1-acetyl-1,2,3,6-tetrahydro-pyridin-4-yl)-4-methoxy-benzothiazol-2-yl]-4-fluoro-benzamide as an off-white solid; F.p.: 264-265° C.

1. customAt 0° C
2. additionwere added
3. extractionAfter extracting with four times 25 ml ethyl acetate the combined organic phases
4. dry with materialwere dried over sodium sulfate
5. concentrationconcentrated to dryness in vacuo