反应详情

A solution of 1-diphenylmethyl-3-methanesulphonyloxyazetidine (see Preparation 54) (4.8 g, 15.1 mmol) and 1-aminosulphonylpiperazine (see Example 123(f)) (5 g) in acetonitrile (50 ml) was heated under reflux for 4 hours. The reaction was cooled and the solid filtered off and washed with acetonitrile (50 ml). The filtrate was concentrated under reduced pressure and the residue slurried in hot toluene (50 ml), cooled, the solid filtered off and washed with toluene (50 ml). The product was then further purified by slurrying in hot ethyl acetate (3 ml), cooling and filtering to give the title compound (0.47 g).

1. temperatureunder reflux for 4 hours
2. temperatureThe reaction was cooled
3. filtrationthe solid filtered off
4. washwashed with acetonitrile (50 ml)
5. concentrationThe filtrate was concentrated under reduced pressure
6. temperaturethe residue slurried in hot toluene (50 ml), cooled
7. filtrationthe solid filtered off
8. washwashed with toluene (50 ml)
9. customThe product was then further purified
10. temperaturecooling
11. filtrationfiltering