Nucleophilic Phosphine Organocatalysis: a Practical Synthetic Strategy for the Drug-Like Nitrogen Heterocyclic Framework Construction

Nucleophilic phosphine catalysis has proven to be a practical and powerful synthetic strategy in organic chemistry, which can provide easy access to five-, six-, seven-, and eight-membered nitrogen heterocyclic compounds. The reaction topologies can be controlled by a proper choice of the phosphine catalysts, as well as the functionalization of the reaction substrates. In many cases, the reactions take place smoothly at room temperature, with high efficiency and atom economy. This mini-review presents the recent advances in nucleophilic phosphine catalysis for the synthesis of drug-like nitrogen heterocylic compounds. The nitrogen heterocyclic compounds with significant biological activities derived from the library based on nucleophilic phosphine-catalyzed annulation reactions are also highlighted.