AbstractPhenanthridines are a privileged heterocyclic compound that exists in many natural products and has been known to exhibit a variety of pharmacological properties. In the last few decades, an incredible development has taken place to synthesise this scaffold. In this regard, 2‐isocyanobiphenyl has become one of the most exploited substrates that allow the direct formation of phenanthridine derivatives under various novel and conventional methods. The present review provides an overview of synthetic approaches for the preparation of phenanthridine, and their derivatives form 2‐isocyanobiphenyls′′.