Wang You-Qing, Cui Xiao-Yu, Ren Yuan-Yuan, Zhang Yongna
Provincial Key Laboratory of Natural Medicine and Immuno-Engineering, College of Chemistry and Chemical Engineering, Henan University, Kaifeng, Henan 475004, P. R. China.
Org Biomol Chem. 2014 Dec 7;12(45):9101-4. doi: 10.1039/c4ob01902d.
A highly enantioselective direct Mannich reaction of methyl alkyl ketones with cyclic imines benzo[e][1,2,3]oxathiazine 2,2-dioxides, catalyzed by the combination of cinchona alkaloid derived primary amine and TFA, is disclosed. For unsymmetrical methyl alkyl ketones, it is favoured that specific regioselective addition to the imine substrates occurs at the less-substituted methyl group by steric control.
公开了一种由金鸡纳生物碱衍生的伯胺与三氟乙酸组合催化的、甲基烷基酮与环状亚胺苯并[e][1,2,3]恶唑嗪2,2-二氧化物的高度对映选择性直接曼尼希反应。对于不对称甲基烷基酮，通过空间控制，在亚胺底物上的特定区域选择性加成有利于在取代较少的甲基处发生。
