One-Pot Catalytic Enantioselective Synthesis of Tetrahydropyridines via a Nitro-Mannich/Hydroamination Cascade

The highly enantioselective preparation of synthetically useful tetrahydropyridine derivatives employing a one-pot nitro-Mannich/hydroamination cascade is reported. This approach utilizes an asymmetric organocatalytic nitro-Mannich reaction followed by a gold-catalyzed alkyne hydroamination/isomerization sequence that yields the desired tetrahydropyridines in good yields and high diastereo- and enantioselectivities.

本报道介绍了一种高度对映选择性的合成方法，该方法采用一锅硝基-Mannich/氢氨化级联反应，用于制备具有合成价值的多氢吡啶衍生物。该策略利用了对称有机催化硝基-Mannich反应，随后通过金催化的炔烃氢氨化/异构化序列，以良好的产率和极高的对映异构体选择性和对映选择性，得到所需的四氢吡啶化合物。