Heterocycles are among the well-established classes of compounds, constituting a wide range of organic molecules. These structural motifs not only have a dominant presence in a wide variety of drugs but are also equally present as ubiquitous fragments of numerous vitamins, biologically active natural products, biomolecules, and synthetic drug candidates. Their key role in medicinal chemistry in the design of safe, effective, and efficacious drug molecules gives an impetus to the scientific community to access heterocyclic entities from robust chemical reactions. In this review, we summarize a diverse range of synthetic methods employing alkynoates as key starting materials to furnish useful bioactive heterocyclic frameworks (nitrogen, oxygen, sulfur, fused- and hetero-spirocycles), thus offering new opportunities and expanding the toolbox of synthetic chemistry reactions under transition-metal-free conditions. Several reaction parameters such as the use of easily available starting materials, commercially accessible reagents, and ease of synthesis (moderate temperatures, short reaction times, high yields, limited by-products) are included in the discussion alongside the reaction scope and limitations as well as mechanistic insights. The application of these methodologies in the synthesis of natural products and pharmaceuticals has also been discussed. We hope that the diverse utilities of alkynoates in the delivery of various heterocycles will fulfil the objectives of medicinal chemists in overcoming the formidable challenges associated with drug discovery and development.

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烷酸酯类无过渡金属合成杂环的新领域：概述和现状

杂环是成熟的化合物类别，构成广泛的有机分子。这些结构基序不仅在多种药物中占主导地位，而且还以多种维生素，生物活性天然产物，生物分子和合成药物候选物的普遍存在形式存在。它们在药物化学中设计安全，有效和有效的药物分子中的关键作用，推动了科学界从强大的化学反应中获得杂环实体的动力。在这篇综述中，我们总结了多种多样的合成方法，其中以炔酸为主要原料提供有用的生物活性杂环骨架（氮，氧，硫，稠合和杂螺环），因此提供了新的机会，并扩大了在无过渡金属条件下合成化学反应的工具箱。除了反应范围和限制外，讨论中还包括几个反应参数，例如使用容易获得的起始原料，可商购的试剂以及易于合成（温度适中，反应时间短，产率高，副产物有限）。机械的见解。还讨论了这些方法在天然产物和药物合成中的应用。我们希望炔烃在各种杂环的递送中的各种效用将实现药物化学家克服与药物发现和开发相关的巨大挑战的目标。