Carbonylative Construction and Transformation of Strained Carbocycles

High Resolution Image Download MS PowerPoint Slide Strained carbocycles such as cyclopropanes and cyclobutanes are privileged motifs in modern medicinal chemistry, which have also been verified by the over 20 strained carbocycle-containing drugs approved by the FDA between 2015 and 2019. Moreover, owing to their high intrinsic strain and distinctive reactivity, these small-ring carbocycles have become indispensable building blocks in synthetic chemistry. Carbonylation reactions employing carbon monoxide (CO) as a versatile C1 synthon offer efficient access to structurally diverse and industrially relevant carbonyl-containing compounds. Recent advances have consequently unveiled a powerful synergy between ring strain and carbonylation. Under these backgrounds, this review provides a systematic overview of developments from 2000 to 2025, with a focus on carbonylative cyclopropanation with CO and strain-release carbonylative transformations of strained carbocycles. By summarizing representative transformations and mechanistic trends, we furthermore highlight emerging opportunities in catalyst design, selectivity control, and synthetic applications.