反应详情

EDC (109.3 mg, 0.5704 mmol) was added to a stirred suspension of [[3-amino-6-(4-isopropylsulfonylphenyl)pyrazine-2-carbonyl]amino]thiourea (150 mg, 0.3803 mmol) in DCE (3.000 mL) and the reaction mixture heated at reflux for 22 h. The solvent was removed in vacuo and the residue partitioned between EtOAc and water. The aqueous layer was extracted with EtOAc (3×10 mL) and the combined organic extracts dried MgSO4, filtered and concentrated in vacuo to give the sub-title compound as a yellow solid (118 mg, 86%) 1H NMR (400 MHz, DMSO) d 1.19 (d, 6H), 3.45 (dt, 1H), 7.65-7.80 (m, 4H), 7.95 (d, 2H), 8.26 (d, 2H) and 8.89 (s, 1H) ppm; MS (ES+) 361.0

1. temperaturethe reaction mixture heated
2. temperatureat reflux for 22 h
3. customThe solvent was removed in vacuo
4. customthe residue partitioned between EtOAc and water
5. extractionThe aqueous layer was extracted with EtOAc (3×10 mL)
6. filtrationthe combined organic extracts dried MgSO4, filtered
7. concentrationconcentrated in vacuo