噁唑骨架的高效构建策略

罗倩婷; 种雪兰; 焦丽萍; 吴秀敏; 何华锋

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罗倩婷,种雪兰,焦丽萍,吴秀敏,何华锋.化学通报,2025,88(12):1288-1297.

噁唑骨架的高效构建策略

Strategies for Efficient Construction of Oxazole Skeletons

投稿时间：2025-06-18 修订日期：2025-09-15

DOI：

中文关键词: 噁唑酰胺氮杂环氰基合成策略

英文关键词:Oxazole, Amide, Azacycle, Cyano group, Synthetic strategy

基金项目:

作者	单位	E-mail
罗倩婷	^{山东第一医科大学}山东省科学院药学院药物研究所济南	luoqianting2024@163.com
种雪兰	^{济宁医学院药学院日照}
焦丽萍	^{济宁医学院药学院日照}
吴秀敏	^{济宁医学院药学院日照}
何华锋^*	^{济宁医学院药学院日照}	captainhuafeng@mail.jnmc.edu.cn

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中文摘要:

噁唑骨架是广泛存在于多种天然产物和活性药物的重要结构片段，其独特的杂原子结构和芳香性，使其具备卓越的生物活性。近年来，大量噁唑骨架构建的新颖策略被报道披露。为更好指导相关研究，激发创新性反应策略开发，制备结构新颖、活性突出的噁唑类药物前体，文章系统梳理近期有关噁唑骨架构建的报道，依据噁唑骨架中氮原子的来源，分别总结归纳了酰胺、氰基/异氰基、胺类及含氮杂环等含氮前体基团高效构建噁唑的报道，并探讨研究中所存在的问题与挑战,在文献报道和深入分析的基础上，推导预测了噁唑环构建的潜在反应机理。进一步，指出后续围绕噁唑骨架及其衍生物的化学合成、绿色催化体系设计、精准机理解析以及特异生物活性筛选等方向仍具有重要的研究潜力与现实需求。

英文摘要:

The oxazole scaffold is a crucial structural motif widely found in various natural products and bioactive pharmaceutical compounds. Its unique heteroatomic framework and aromaticity endow it with remarkable biological activity. In recent years, numerous novel strategies in construction of oxazole scaffold have been disclosed. Advances were summarized systematically in order to be benefit for related research. As well, development of innovative synthetic methodologies for construction of oxazole would be inspired. In addition, more oxazole-based drug precursors with novel structure and bioactivities could be prepared. According to the source of nitrogen within the oxazole ring, the review was proposed in line with the precursors employed in the documents, etc. amides, cyano/isocyanate groups, amines, and nitrogen-containing heterocycles. Furthermore, potential reaction mechanisms for the formation of oxazole ring were deduced and proposed based on comprehensive literature analysis. Meanwhile, challenges and limitations waiting to be resolved in the area of assembling of oxazole were also analyzed. On the basis, chemical synthesis of oxazole scaffolds and their derivatives, design of green catalytic system, elucidation of the precise mechanism, and the screening of specific biological activities were highlighted as the continued significance and practical demand in related to studies on oxazole in future.

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