反应详情

Mix 3-[4-(1,1-difluoroethyl)phenyl]isothiazol-5-ylamine (0.200 g, 0.833 mmol), benzyl (R,R)-2-methylcyclopropanecarboxylate (0.238 g, 1.250 mmol) and potassium t-butoxide (0.190 g, 1.667 mmol) for 1 h. Dilute with satd NaHCO3 and extract with EtOAc. Wash the organic phase with brine, dry (MgSO4) and evaporate. Chromatography on silica gel, eluting with 10% EtOAc in CHCl3, affords (R,R)—N-[3-[4-(1,1-difluoroethyl)phenyl]isothiazol-5-yl]-2-methylcyclopropane-carboxamide. Yield: 50.3%. ES-MS: m/e 323.3 (m+1).

1. extractionextract with EtOAc
2. washWash the organic phase with brine
3. dry with materialdry (MgSO4)
4. customevaporate
5. washChromatography on silica gel, eluting with 10% EtOAc in CHCl3