反应详情

To a solution of 2-[({[(1-methyl-1H-imidazol-5-yl)(phenyl)methylene]amino}oxy)methyl]-pyrimidin-4-amine (200 mg, 0.65 mmol) in 1,4-dioxane (10 mL) were sequentially added triethylamine (0.18 mL, 1.30 mmol) and cyclopropanecarboxylic acid (0.24 mL, 2.60 mmol). After stirring at room temperature for 24 h, the mixture was concentrated in vacuo, diluted in ethyl acetate (50 mL), washed with water (20 mL), dried over MgSO4 and concentrated to dryness in vacuo. Purification on silica gel afforded N-(cyclopropylcarbonyl)-N-{2-[({[(1-methyl-1H-imidazol-5-yl)(phenyl)methylene]amino}oxy)methyl]pyrimidin-4-yl}cyclopropanecarboxamide [23 mg, yield 8%; HPLC/MS: m/z=445 (M+H); log P(HCOOH)>=1.75].

1. concentrationthe mixture was concentrated in vacuo
2. additiondiluted in ethyl acetate (50 mL)
3. washwashed with water (20 mL)
4. dry with materialdried over MgSO4
5. concentrationconcentrated to dryness in vacuo
6. customPurification on silica gel