反应详情

A solution of tert-butyl (3R)-6-cyclohexyl-3-{3-[(methylamino)methyl]-1,2,4-oxadiazol-5-yl}hexanoate (preparation 5) (300 mg, 0.82 mmol) in pyridine (2 ml) in a water bath was treated with methanesulphonylchloride (64 μl, 0.82 mmol) and stirred under a nitrogen atmosphere for 20 minutes. The solvent was removed under reduced pressure. The residue was dissolved in EtOAc and washed with 2M HCl followed by brine. The organic extract was dried over MgSO4, filtered and the solvent removed under reduced pressure. The residue was purified on a silica column eluting with a solvent gradient of EtOAc:pentane (5:95) gradually changing to (30:70) to afford the title compound as a colourless oil (273 mg, 75%).

1. customThe solvent was removed under reduced pressure
2. dissolutionThe residue was dissolved in EtOAc
3. washwashed with 2M HCl
4. extractionThe organic extract
5. dry with materialwas dried over MgSO4
6. filtrationfiltered
7. customthe solvent removed under reduced pressure
8. customThe residue was purified on a silica column
9. washeluting with a solvent gradient of EtOAc:pentane (5:95)