反应详情

To a solution of 0.75 g (0.165 mMol) N-(4-methoxy-7-piperidin-4-yl-benzothiazol-2-yl)-2-methyl-isonicotinamide hydrochloride (1:2) in 4 ml THF were added 0.05 ml triethyl amine. At 0° C. 0.019 ml (0.2 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. A precipitation formed, which was filtered. The residue on the filter was triturated in water. Upon isolation and drying in vacuo one obtained 0.052 g (74%) N-[7-(1-acetyl-piperidin-4-yl)-4-methoxy-benzothiazol-2-yl]-2-methyl-isonicotinamide as a white solid. F.p.: 213-215° C.

1. customAt 0° C
2. additionwere added
3. customA precipitation
4. customformed
5. filtrationwhich was filtered
6. customThe residue on the filter was triturated in water
7. customUpon isolation and drying in vacuo one