反应详情

To tert-butyl (6R,7S)-6-(acetylamino)-7-(3,4-dichlorophenyl)-1,4-oxazepane-4-carboxylate (200 mg) was added 4.0 M hydrogen chloride-ethyl acetate solution (4 mL), and the mixture was stirred at room temperature for 1 hr. The residue obtained by concentration under reduced pressure was desalted by a solid phase extraction resin (column: PL StrastoSphere solid phase extraction resin (PL-HCO3 MP StratoSpheres™), 500 mg, StrastoSphere, mobile phase: methanol). To a solution of the residue obtained by concentration under reduced pressure in ethanol was added a solution of fumaric acid (33.7 mg) in ethanol. The mixture was concentrated under reduced pressure to give the title compound (130 mg).

1. customThe residue obtained by concentration under reduced pressure
2. extractionwas desalted by a solid phase extraction resin (column
3. extractionPL StrastoSphere solid phase extraction resin (PL-HCO3 MP StratoSpheres™), 500 mg
4. customTo a solution of the residue obtained by concentration under reduced pressure in ethanol
5. concentrationThe mixture was concentrated under reduced pressure