反应详情

To a solution of 0.05 g (0.095 mMol) N-(4-methoxy-7-piperidin-4-yl-benzothiazol-2-yl)-2-morpholin-4-yl-isonicotinamide 1:2 hydrochloride in 3 ml THF were added 0.029 ml triethyl amine. At 0° C. 0.011 ml (0.11 mMol) acetic anhydride was added dropwise and stirred for 1 h. Then a mixture of 5 ml sat. aqueous sodium bicarbonate and 10 ml water were added. This was extracted three times with 15 ml ethyl acetate, the combined organic phase were dried over sodium sulfate and evaporated to dryness in vacuo. One obtained 0.031 g (66%) N-[7-(1-acetyl-piperidin-4-yl)-4-methoxy-benzothiazol-2-yl]-2-morpholin-4-yl-isonicotinamide as a white solid. F.p.: 231-233° C.

1. customAt 0° C
2. additionwere added
3. extractionThis was extracted three times with 15 ml ethyl acetate
4. dry with materialthe combined organic phase were dried over sodium sulfate
5. customevaporated to dryness in vacuo