反应详情

4-Chloro-5-fluoro-2-{[(1R)-3-iodo-1-phenylpropyl]oxy}benzonitrile (200 mg, 0.48 mmol), 5-methyl-2-pyrazinemethanamine (120 mg, 0.96 mmol) and triethylamine (335 μl, 2.4 mmol) were stirred in DMSO (5 ml) for 48 h. The mixture was washed with water and purified by chromatography (5% 1M ammonia-methanol/dichloromethane). The eluent was evaporated and the residue treated with 4M hydrogen chloride in dioxan (5 ml). The solvent was evaporated, azeotroped twice with toluene and triturated with ether to give the required product as a white solid.

1. washThe mixture was washed with water
2. custompurified by chromatography (5% 1M ammonia-methanol/dichloromethane)
3. customThe eluent was evaporated
4. additionthe residue treated with 4M hydrogen chloride in dioxan (5 ml)
5. customThe solvent was evaporated
6. customazeotroped twice with toluene
7. customtriturated with ether