反应详情

To a solution of 1-diphenylmethyl-3-methanesulphonyloxyazetidine (WO 96/05193) (1.4 g) in dioxane (25 mL) were added N-methyl benzenesulphonamide (1.2 g) and caesium carbonate (2.6 g). The reaction mixture was heated to reflux for 3 h, then cooled to room temperature. Water (20 mL) was added to the resulting slurry, and the mixture was extracted with ethyl acetate (3×25 mL). The combined organics were washed with brine, dried over magnesium sulphate, filtered and dried in vacuo to yield crude product. Chromatography on silica gel eluting with ethyl acetate:hexanes (2:3 by volume) yielded the title compound as a white foam (1.31 g).

1. temperatureThe reaction mixture was heated
2. temperatureto reflux for 3 h
3. extractionthe mixture was extracted with ethyl acetate (3×25 mL)
4. washThe combined organics were washed with brine
5. dry with materialdried over magnesium sulphate
6. filtrationfiltered
7. customdried in vacuo
8. customto yield crude product