反应详情

100 mg of 2-cyano-3-fluoro-benzenesulfonyl chloride (EP33984 A1 19810819) is added to a solution of 0.85 ml of cyclopropylmethylamin in 3.5 ml of THF. After stirring for 3 hours at room temperature the reaction mixture is poured into water. The mixture is acidified with hydrochloric acid (˜pH3) and extracted three times with methylenchloride. The combined organic phases are dried (Na2SO4), filtered and concentrated. Preparative HPLC affords 16 mg of 4-fluoro-2-cyclopropylmethyl-1,2-benzisothiazol-3(2H)-imine 1,1-dioxide as an orange solid (m.p. 90-93° C.).

1. extractionextracted three times with methylenchloride
2. dry with materialThe combined organic phases are dried (Na2SO4)
3. filtrationfiltered
4. concentrationconcentrated