反应详情

To a solution of 3-oxa-7,9-diaza-bicyclo[3.3.1]nonane-9-carboxylic acid benzyl ester (Compound X) (100 mg, 0.33 mmol) in CH2Cl2 (5 mL) was added DIPEA (0.23 mL, 1.32 mmol) and methanesulfonyl chloride (57 mg, 0.49 mol). The reaction mixture was stirred at room temperature for 1 hour, and then quenched with sat. NH4Cl, then diluted with EtOAc (60 mL). The mixture was washed with sat. NH4Cl, sat. NaHCO3 and brine (20 mL) respectively. The organic layer was dried over Na2SO4. The solvent was removed under reduced pressure to give 7-methanesulfonyl-3-oxa-7,9-diaza-bicyclo[3.3.1]nonane-9-carboxylic acid benzyl ester (Compound Y) (105 mg, 95%) as yellowish oil. MS: calc'd (MH+) 341, measured (MH+) 341.

1. customquenched with sat. NH4Cl
2. additiondiluted with EtOAc (60 mL)
3. washThe mixture was washed with sat. NH4Cl, sat. NaHCO3 and brine (20 mL) respectively
4. dry with materialThe organic layer was dried over Na2SO4
5. customThe solvent was removed under reduced pressure