反应详情

Ammnonium formate (0.316 g, 5 mmol) is added to a solution of [2-(5-ethyl-oxazol-2-yl)-ethyl]-carbamic acid benzyl ester (step 3) (1.66 mmol) in methanol (15 ml) and 10% Pd on carbon (125 mg) is added under an inert atmosphere. The mixture is stirred at ambient temperature for 2 hours. The catalyst is removed by filtration and the filtrate is evaporated. The residue is diluted with dichloromethane, filtered to remove undissolved solid and the solvent is removed. The residue is dissolved in DCM and treated with 1M aqueous sodium hydroxide solution (5 ml). The organic extract is separated, dried (MgSO4), filtered and the solvent is removed. Crystallisation from ethyl acetate/dichloromethane affords the titled compound.

1. additionis added under an inert atmosphere
2. customThe catalyst is removed by filtration
3. customthe filtrate is evaporated
4. additionThe residue is diluted with dichloromethane
5. filtrationfiltered
6. customto remove undissolved solid
7. customthe solvent is removed
8. dissolutionThe residue is dissolved in DCM
9. additiontreated with 1M aqueous sodium hydroxide solution (5 ml)
10. extractionThe organic extract
11. customis separated
12. dry with materialdried (MgSO4)
13. filtrationfiltered
14. customthe solvent is removed
15. customCrystallisation from ethyl acetate/dichloromethane