反应详情

温度

80 °C

A flask was charged with 4-nitro-1H-pyrazole (3.5 g, 30.02 mmol), 2-(boc-amino)ethylbromide (6.9 g, 30.02 mmol), Cs2CO3 (1.07 g, 33.02 mmol) and MeCN (60 mL). The resulting reaction mixture was stirred at reflux (80° C.) for 1.5 h, then allowed to reach rt. The mixture was diluted with DCM, filtered, the filter cake was washed with DCM. The filtrate was concentrated to yield tert-butyl(2-(4-nitro-1H-pyrazol-1-yl)ethyl)carbamate as a light orange oil, which was used in the next step without further purification. LC-MS conditions B: tR=0.63 min, [M+H]+=257.35.

1. customThe resulting reaction mixture
2. customto reach rt
3. filtrationfiltered
4. washthe filter cake was washed with DCM
5. concentrationThe filtrate was concentrated