Atropisomeric molecules are privileged scaffolds, not only as ligands for asymmetric synthesis, but also as biologically active products and advanced materials. Although very attractive from a sustainability viewpoint, the direct construction of the stereogenic axis through asymmetric C–H arylation is very challenging and consequently only a few examples have been reported. This short review summarizes these very recent results on the atropo-enantio or diastereo­selective synthesis of atropisomeric (hetero)biaryl molecules; transformations during which the Ar–Ar atropisomeric axis is formed during the C–H activation process.

1 Introduction

2 Atropo-enantioselective Intermolecular Pd-Catalyzed C–H Arylation of Thiophene Derivatives

3 Atropodiastereoselective Intermolecular Pd-Catalyzed C–H Arylation towards Terphenyl Scaffolds Bearing Two Atropisomeric Axes

4 Atropo-enantioselective Intramolecular Pd-Catalyzed C–H Arylation towards Atropisomeric Benzodiazepinones

5 Atropo-enantioselective Intermolecular Pd-Catalyzed C–H Arylation of Heteroarenes

6 Rh-Catalyzed Atropo-enantioselective C–H Arylation of Diazonaphthoquinones

7 Conclusion

阻转异构分子是特权的支架，不仅作为不对称合成的配体，而且还作为生物活性产物和高级材料。尽管从可持续性的角度来看非常有吸引力，但是通过不对称的C–H芳基化直接构建立体轴的方法非常具有挑战性，因此仅举了几个例子。这篇简短的综述总结了对阻转异构（杂）联芳基分子的对映异构或非对映选择性合成的最新结果。在C–H活化过程中形成Ar–Ar阻转异构体轴的转变。

1引言

2噻吩衍生物的对映体对映选择性分子间钯催化的C–H芳基化

3对具有两个对映异构体轴的三联苯骨架的对映体选择性Pd分子间Pd催化的C–H芳基化

4对对映异构体苯并二氮杂A酮的对映体对映选择性分子内钯催化的C–H芳基化

5杂芳烃的对映体对映选择性分子间钯催化的CH芳基化

6 Rh催化的重氮萘醌的对映体对映体选择性C–H芳基化

7结论