反应详情

3-(3-(Trifluoromethyl)phenylamino)cyclopent-2-enone (234 mg, 0.97 mmol) is added to a solution of 4-bromo-1-(chloro(isocyanato)methyl)-2-(methylsulfonyl)benzene (Step 1, 945 mg, 2.91 mmol) in dichloromethane (10 mL). The mixture is heated at reflux over night and then concentrated under reduced pressure. The residue is purified by reversed phase HPLC (Agilent ZORBAX™ SB—C18, gradient of acetonitrile in water, 0.1% formic acid). Yield: 110 mg; ESI mass spectrum: ESI mass spectrum: [(79Br)-M+H]+=529, [(81Br)-M+H]+=531; Retention time HPLC: 1.21 min (Z017_S04).

1. temperatureThe mixture is heated
2. temperatureat reflux over night
3. concentrationconcentrated under reduced pressure
4. customThe residue is purified by reversed phase HPLC (Agilent ZORBAX™ SB—C18, gradient of acetonitrile in water, 0.1% formic acid)
5. custom1.21 min (Z017_S04)