有机催化丙二酸酯与β-硝基烯烃的不对称Michael加成反应

Organocatalyzed asymmetric Michael reaction of malonates withβ-nitroolefins

将金鸡纳生物碱衍生物用于催化丙二酸酯和β-硝基芳基乙烯的不对称Michael加成反应。考察溶剂、温度及催化剂用量对反应催化性能的影响。结果表明,最佳催化条件为5 mol%催化剂1e,甲苯为溶剂,0℃反应。得到了86~93%的化学产率和最高达99%ee的对映选择性。

Cinchona alkaloid derivatives as organocatalysts were applied in asymmetric Michael addition of malonates withβ-nitroolefins.The effect of solvent,temperature and catalyst loading amount were investigated.The optimized conditions were determined with toluene as the solvent with 5 mol%loading of catalyst 1 e at 0℃.The desired products were obtained in 86~93%yield with up to 99%ee.