3‐Component Approach to 1,5‐Dihydro‐2 H ‐pyrrol‐2‐one Heterocycles

Abstract

Abstract This chapter presents the procedure for the 3‐component approach to 1,5‐Dihydro‐2H‐pyrrol‐2‐one heterocycles. Nitrogen‐containing heterocycles (N‐heterocycles) are a commonality among bioactive natural products often represented in alkaloids and other privileged scaffolds. A frequently observed motif is a 5‐membered N‐heterocycle, present in indoles, pyrroles, pyrrolidines and succinimides. The niche of 5‐membered nitrogen containing heterocyclic natural products has supplied potent anticancer therapies such as vinblastine, as well as treacherous poisons such as strychnine. In summary, N‐heterocycles such as pyrrolidinones have shown to be of significant relevance in the pharmaceutical and fine chemical industry. Furthermore, their extensive presence in natural products makes it of high importance to develop scalable, efficient, and modular approaches to pyrrolidone cores. The procedure described herein provides an attractive means to synthesize highly functionalized pyrrolidinones.