反应详情

A mixture of N-cyclobutyl-1,6-naphthyridine-2-carboxamide (227 mg, 1 mmol), tert-butyl bromoacetate (234 mg, 1.2 mmol) in CH3CN (15 mL) is refluxed overnight. Solvent is removed in vacuo and the residue is dissolve in MeOH (20 mL). To the solution is added NaBH4 (181 mg, 4.8 mmol) and the mixture is refluxed for 4 hr. The solvent is removed in vacuo and the residue is partitioned between water (20 mL) and EtOAc (20 mL). The layers are separated and the aqueous layer is extracted with EtOAc (20 ml). The combined extracts are washed with brine (10 mL), dried and evaporated. The residue is purified by flash column to give the title compound as a light yellow oil. MS (M+1): 346.2.

1. temperatureis refluxed overnight
2. customSolvent is removed in vacuo
3. dissolutionthe residue is dissolve in MeOH (20 mL)
4. temperaturethe mixture is refluxed for 4 hr
5. customThe solvent is removed in vacuo
6. customthe residue is partitioned between water (20 mL) and EtOAc (20 mL)
7. customThe layers are separated
8. extractionthe aqueous layer is extracted with EtOAc (20 ml)
9. washThe combined extracts are washed with brine (10 mL)
10. customdried
11. customevaporated
12. customThe residue is purified by flash column