反应详情

温度

40 °C

A mixture of 2-chloro-6-(methyloxy)-3-nitropyridine (1.9 g, 10 mmol), 1,1-dimethylethyl [1-(2-aminoethyl)-4-piperidinyl]carbamate (2.43 g, 10 mmol) and potassium carbonate (1.4 g, 10 mmol) in acetonitrile (35 ml) and DMF (10 ml) was heated at 40° C. for 30 minutes. The mixture was filtered, washing with acetonitrile, and evaporated. The residue was dissolved in the minimum volume of DCM (15 ml) and washed with water (1 ml). The organic extract was added to a silica column which was then eluted with 0-100% ethyl acetate in hexane affording a yellow solid (3.1 g, 78%).

1. filtrationThe mixture was filtered
2. washwashing with acetonitrile
3. customevaporated
4. dissolutionThe residue was dissolved in the minimum volume of DCM (15 ml)
5. washwashed with water (1 ml)
6. extractionThe organic extract
7. additionwas added to a silica column which
8. washwas then eluted with 0-100% ethyl acetate in hexane affording a yellow solid (3.1 g, 78%)