Review reveals diverse cycloadditions for synthesizing nitrogen-containing heterocycles, indicating new pathways for medicinal chemistry.
1,1‐Disubstituted vinyl bromides have emerged as powerful and versatile building blocks for the synthesis of nitrogen‐containing heterocycles. Their dual functionality—encompassing both a reactive bromide and a polarized CC bond—enables diverse transformations including cycloadditions, metal‐catalyzed couplings, lithiation, and radical or cascade processes. This review summarizes recent advances up to 2025 in the preparation of aziridines, pyrroles, indoles, indolizines, pyrrolidines, pyrazoles, triazoles, isoxazoles, isoxazolidines, and piperidines derived from these substrates. Particular attention is given to regio‐ and stereoselective strategies, the construction of fluorinated and functionalized heterocycles, and applications in medicinal chemistry.
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Westermeyer et al. (2026) studied this question.
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