反应详情

To a stirred solution of biphenyl-2-ylcarbamic acid 1-{2-[(4-hydroxymethyl-2-methoxybenzoyl)methylamino]ethyl}piperidin-4-yl ester (78 mg, 1.5 mmol; prepared as described in Preparation 20) in DCM (2.5 mL) at −15° C. was added DMSO (130 μL, 22.5 mmol), and DIPEA (130 μL, 7.5 mmol). To the solution was added sulfur trioxide-pyridine complex (240 mg, 15 mmol). After 30 minutes, the reaction mixture was quenched with water (˜3 mL). Two layers were separated, the organic layer was dried over MgSO4, filtered and the title intermediate was used directly in the next reaction.

1. additionTo the solution was added sulfur trioxide-pyridine complex (240 mg, 15 mmol)
2. customthe reaction mixture was quenched with water (˜3 mL)
3. customTwo layers were separated
4. dry with materialthe organic layer was dried over MgSO4
5. filtrationfiltered
6. customthe title intermediate was used directly in the next reaction