Sep 2026· Annalen der Pharmacie· 0 citations· 148 references
Abstract
Cyclobutane‐fused heterocycles represent a distinctive class of structurally constrained scaffolds with significant relevance in natural products and medicinal chemistry. Recent advances in synthetic organic chemistry have enabled the development of diverse, increasingly efficient strategies for their construction. Among these, [2 + 2] cycloaddition‐based approaches have emerged as central tools, spanning photochemical dearomative transformations of heteroarenes, olefin [2 + 2] photocycloadditions, and Lewis acid‐ or transition‐metal‐catalyzed variants, including enantioselective and visible‐light‐mediated processes. Alongside these approaches, complementary ring‐closure strategies, including cascade processes and strain‐release annulations, have also been reported in recent years, providing efficient and elegant access to cyclobutane‐fused heterocycles through mechanistically distinct pathways. This review provides a critical overview of the principal synthetic strategies for constructing cyclobutane‐fused heterocycles, with an emphasis on reactivity patterns, selectivity control, and mechanistic features.
The last decade has witnessed a remarkable transformation in alkoxyallene chemistry. Although historically employed as synthetic equivalents of acrolein or as versatile 3C synthons, alkoxyallenes are now increasingly recognized as highly adaptable platforms for synthetic design. The combination of a polarized cumulene...
A. Lanfranco, M. Rusconi, J. Saglietto et al.· Advanced Synthesis & Cat...· 0 citations
α‐Diazocarbonyl compounds, as a class of versatile organic synthons, occupy a pivotal position in the field of organic chemistry. Their unique structural features endow them with rich reactivity, enabling decomposition under thermal, photolytic, or transition‐metal‐catalyzed conditions to generate highly reactive carbe...
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Thiazole is a versatile sulfur‐ and nitrogen‐containing heterocycle that occupies a prominent position in medicinal, natural‐product, and materials chemistry. Its highly tunable structure is found in numerous bioactive natural products and pharmaceuticals, while thiazole derivatives exhibit diverse biological activit...
Diazirines are three‐membered nitrogen‐containing heterocycles best known as photochemical carbene precursors in photoaffinity labeling. Upon irradiation, diazirines undergo nitrogen extrusion to generate highly reactive carbenes capable of covalent bond insertion, a property that has been widely exploited in chemical...
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Imidazo[1,2‐
a
]pyridines and imidazo[1,2‐
a
]pyrazines are important nitrogen‐containing heterocycles with applications in medicinal and materials chemistry. Herein, we report a regioselective synthetic strategy for the preparation of novel diaza‐ and triazadibenzoazulene derivatives through sequential Pd‐cataly...
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