反应详情

To a solution of 2,3-difluoronitrobenzene (5.0 g, 31 mmol) in EtOH (25 mL) were added tert-butyl piperidin-4-ylmethylcarbamate (8.1 g, 38 mmol), and N,N-diisopropylethylamine (6.6 mL, 38 mmol). The reaction was irradiated to 110° C. for 20 min by microwave. The crude reaction mixture was diluted with EtOAc, washed with 1 N HCl and brine, dried over MgSO4 and concentrated to yield nitrobenzene Int-2a (11.2 g, 99%) as yellow crystals. The crude product was used without further purification.

1. customThe reaction was irradiated to 110° C. for 20 min by microwave
2. customThe crude reaction mixture
3. washwashed with 1 N HCl and brine
4. dry with materialdried over MgSO4
5. concentrationconcentrated