Carbonylation: Unlocking Opportunities for Bioactive Molecule and Pharmaceutical Development

Abstract

Bioactive small molecules play indispensable roles in diverse biological processes, while isotope-labeled analogues are frequently employed as chemical probes to elucidate complex biochemical pathways. Consequently, synthetic chemistry holds a central position in both pharmaceutical research and the life sciences. Methodologies in synthetic chemistry, together with the total synthesis of natural products, serve as essential tools, providing diverse chemical libraries for the discovery and development of bioactive agents. Meanwhile, carbonyl scaffolds are ubiquitously found in natural products and therapeutic molecules, rendering the rapid and efficient construction of carbonyl motifs a longstanding challenge in modern synthetic chemistry. This review highlights recent advances in carbonylation strategies that enable the efficient transformation of inexpensive and readily available carbon monoxide and13C-labeled CO precursors into carbonyl-containing bioactive molecules, natural products, and pharmaceuticals.