浅谈Buchwald反应及其在有机合成中的应用

Buchwald Reaction and its Application in Organic Synthesis

钯催化和碱存在下胺与芳基卤化物的交叉偶联反应,产生C-N键,生成胺的N-芳基化产物的反应称为Buchwald反应。因为Buchwald反应中Pd催化剂反应催化交叉耦合反应的联苯二烷基膦配体类型,具有很强的电子、大电阻的这些特征,可以加速氧化增加和减少的循环,因此,即使对底物的活化性差,使用这类配体,也可以在催化剂的量小,时间短,较温和的反应条件,才能获得良好的效果。随着对金属催化反应机理的研究,开发出更多类型的配体,为金属催化交叉偶联反应的发展进程做了极大地推动。由于反应条件温和,化学选择性高而被广泛应用于复杂的药物和生物活性物质的工业生产有机合成中。

In the presence of palladium catalyst and alkali, the cross coupling reaction between amine and aryl halide produces C-N bond, which is called Buchwald reaction. In Buchwald reaction, the type of biphenyl dialkyl phosphonate ligands, which catalyze the cross coupling reaction of Pd catalyst, has the characteristics of strong electron and large resistance, and can accelerate the increase and decrease of oxidation cycle. Therefore, even if the activation of the substrate is poor, the use of such ligands can also obtain good results under the conditions of small amount of catalyst, short time and mild reaction. With the research on the mechanism of metal catalytic reaction, more types of ligands have been developed, which has greatly promoted the development of metal catalytic cross coupling reaction. Due to the mild reaction conditions and high chemical selectivity, it is widely used in the industrial production and organic synthesis of complex drugs and bioactive substances.