反应详情

To a suspension of 4-[6-{[(1,1-dimethylethyl)oxy]carbonyl}-5,6,7,8-tetrahydropyrazolo[3,4-d]azepin-2(4H)-yl]benzoic acid (may be prepared as described in Description 23) (185 mg, 0.52 mmol) in dichloromethane (10 ml) was added 1,1′-(oxomethanediyl)bis-1H-imidazole (168 mg, 1.04 mmol) and the reaction stirred at room temperature, under argon, overnight. Methylamine (64 mg, 2.07 mmol) was added and stirring continued, under argon, at room temperature for 4 hours. The resulting crude mixture was diluted with water, and extracted with dichloromethane (×2). The combined organic fractions were washed with water (×1), dried over magnesium sulphate and solvent evaporated in vacuo to afford the title compound (D24). MS (ES+) m/e 371 [M+H]+.

1. stirringstirring continued, under argon, at room temperature for 4 hours
2. extractionextracted with dichloromethane (×2)
3. washThe combined organic fractions were washed with water (×1)
4. dry with materialdried over magnesium sulphate and solvent
5. customevaporated in vacuo