反应详情

A solution of N-[(2-chloro-3,4-difluorophenyl)methyl]-3-methyl-2-oxo-4-imidazolidinecarboxamide (152 mg, 0.5 mmol) (prepared as described in Example 28), (4-methyl-1H-imidazol-5-yl)methanol hydrochloride (93 mg, 0.625 mmol) and p-toluene sulfonic acid monohydrate (19 mg, 0.100 mmol) in N-methyl-2-pyrrolidone (1 ml) was heated at 130° C. under argon for 3 h. The reaction mixture was cooled to room temperature and diluted with dichloromethane. The solution was washed with saturated sodium hydrogen carbonate solution and brine, dried and evaporated. The residue was purified by mass-directed automated HPLC, followed by trituration with ether to give N-[(2-chloro-3,4-difluorophenyl)methyl]-3-methyl-1-[(4-methyl-1H-imidazol-5-yl)methyl]-2-oxo-4-imidazolidinecarboxamide (147 mg, 74%). LC/MS [M+H]+=398, retention time=1.57 minutes.

1. washThe solution was washed with saturated sodium hydrogen carbonate solution and brine
2. customdried
3. customevaporated
4. customThe residue was purified