反应详情

To a solution of 1-(3-bromo-5-cyanophenyl)piperidine-4-carboxylic acid (1.1 g, 3.6 mmol) in toluene (4 mL) and methanol (2 mL) was added TMSCHN2 (2 M in Et2O, 3.5 mL, 7.0 mmol) dropwise at room temperature. After 1 h, the reaction was quenched with acetic acid (˜0.1 mL), diluted with EtOAc and washed with saturated aqueous NaHCO3. The organic layer was separated, dried (MgSO4), and concentrated to give methyl 1-(3-bromo-5-cyanophenyl)piperidine-4-carboxylate in ˜100% yield.

1. customthe reaction was quenched with acetic acid (˜0.1 mL)
2. additiondiluted with EtOAc
3. washwashed with saturated aqueous NaHCO3
4. customThe organic layer was separated
5. dry with materialdried (MgSO4)
6. concentrationconcentrated