反应详情

温度

140 °C

tert-Butyl 3,8-diazabicyclo[3.2.1]octane-8-carboxylate (0.4 g; 1.9 mmol), prepared as described in (J. Med. Chem., (1998) 41, 674), 5-bromo-2-nitropyridine (0.43 g; 2.27 mmol), prepared as described in (J. Am. Chem. Soc., (1945) 67, 668), and triethylamine (0.23 g; 2.27 mmol) in toluene (10 mL) were heated at reflux for 14 hours. After evaporation of the solvent, additional triethylamine (0.23 g) was added and the mixture further heated at 140° C. for 2 hours. The residue was purified on SiO2 (CH2Cl2:EtOAc 9:1) to provide the title compound.

1. customprepared
2. temperaturewere heated
3. temperatureat reflux for 14 hours
4. customAfter evaporation of the solvent, additional triethylamine (0.23 g)
5. additionwas added
6. customThe residue was purified on SiO2 (CH2Cl2:EtOAc 9:1)