A mild and efficient synthesis of primary amines and amides from aldehydes or ketones using a heterogeneous metal catalyst and amine donor is disclosed. The initial heterogeneous metal-catalyzed reaction between the carbonyl and the amine donor components is followed by the addition of a suitable acylating agent component in one-pot, thus providing a catalytic one-pot three-component synthesis of amides. Integration of enzyme catalysis allows for eco-friendly one-pot co-catalytic synthesis of amides from aldehyde and ketone substrates, respectively. The process can be applied to asymmetric synthesis or to the co-catalytic one-pot three-component synthesis of capsaicin and its analogues from vanillin or vanillyl alcohol. A co-catalytic reductive amination/dynamic kinetic resolution (dkr) relay sequence for the asymmetric synthesis of optically active amides from ketones is disclosed. Implementation of a catalytic reductive amination/kinetic resolution (kr) relay sequence produces the corresponding optically active amide product and optical active primary amine product with the opposite stereochemistry from the starting ketones.
本发明公开了一种利用异相
金属催化剂和胺供体从醛或酮温和高效合成
伯胺和酰胺的方法。在羰基和胺供体组分之间进行最初的异相
金属催化反应后,再加入适当的酰化剂组分,从而实现了酰胺的单组分催化合成。结合酶催化,可分别从醛基质和酮基质中以环保方式实现酰胺的单锅共催化合成。该工艺可用于不对称合成,也可用于以
香兰素或
香草醇为原料,在一次催化下
合成辣椒素及其类似物。本发明公开了一种从酮不对称合成光学活性酰胺的共催化还原胺化/动态动力学解析(dkr)中继序列。通过催化还原酰胺化/动力学解析(kr)中继顺序,可生成与起始酮具有相反立体
化学结构的相应光学活性酰胺产物和光学活性
伯胺产物。