反应详情

8-Methoxy-N-propyl-2-aminotetralin (Arvidsson L.-E. et al., J. Med. Chem., 27, 45 (1984) (2 g, 10 mmol), N-(3-iodopropyl)-2,3-dihydro-1,1-dioxo-3-benzisothiazolone (7.5 g), sodium carbonate (2.5 g), and acetonitrile (25 ml) were heated to reflux for 24 hours. After cooling, the solvent was removed in vacuo and the residue placed on a flash silica gel column (3 cm×35 cm) and eluted with ethyl acetate/hexane (5:95, 10:90, 15:85, 20:80, successively). Solvent removal in vacuo afforded the title compound as a white powder (m.p. 131° C.).

1. temperatureto reflux for 24 hours
2. temperatureAfter cooling
3. customthe solvent was removed in vacuo
4. washeluted with ethyl acetate/hexane (5:95, 10:90, 15:85, 20:80
5. customSolvent removal in vacuo