反应详情

To the solution of 2-(4-tert-butyl-cyclohexyloxy)-quinoline-6-carbaldehyde (350 mg, 1.1 mmol) and piperidine-4-carboxylic acid (145 mg, 1.12 mmol) in ethanol (8 mL, 100 mmol) was heated to reflux for 2 h. The yellow solution was cooled to rt and sodium cyanoborohydride (84.8 mg, 1.35 mmol) was added and was heated to reflux for 1 h. After cooled down to rt, citric acid was added and concentrated down. The solid was suspended in water and filtrate, and the collected solid was washed thoroughly with water. HPLC purification of the solid gives the product. 77 mg, yield: 16%. ESI-MS (M+1)+: 425.00.

1. temperatureto reflux for 2 h
2. temperaturewas heated
3. temperatureto reflux for 1 h
4. temperatureAfter cooled down to rt
5. concentrationconcentrated down
6. washfiltrate, and the collected solid was washed thoroughly with water
7. customHPLC purification of the solid
8. customgives the product