Recent developments in the synthesis of pharmacological alkyl phosphonates

Chenglong Xuan , Zhimin Zhu , Ziyang Li , Chao Shu
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Abstract

Organophosphate analogues are commonly occurring structural features that are widely present in numerous natural substances, biologically active molecules and modern pharmaceutical compounds. The development of efficient strategies for the preparation of these analogues is still attractive but challenging in organophosphorus chemistry. In order to fill this gap, different new routes have been discovered including direct phosphonylation of alkyl radicals, indirect Arbuzov phosphonylation of alkyl radicals and nucleopilic phosphonylation of phosphorus. In this short review, we have attempted to summarize these recent developments for the synthesis of alkyl phosphonates in order to facilitate the development of green pharmacological alkyl phosphonates by emphasizing their variety of products, specificity and relevance, and providing the underlying mechanistic rationale whenever it is possible. We aim to provide readers with a comprehensive understanding of the current state of this field and contribute to future research.

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药用烷基膦酸盐合成的最新进展
有机磷酸酯类似物是一种常见的结构特征,广泛存在于许多天然物质、生物活性分子和现代药物化合物中。在有机磷化学中,高效制备这些类似物的策略的发展仍然具有吸引力,但也具有挑战性。为了填补这一空白,已经发现了不同的新途径,包括烷基自由基的直接磷酸化,烷基自由基的间接Arbuzov磷酸化和磷的亲核磷酸化。在这篇简短的综述中,我们试图通过强调其产品的多样性,特异性和相关性,并尽可能提供潜在的机制原理,来总结烷基膦酸盐合成的最新进展,以促进绿色药理烷基膦酸盐的发展。我们的目标是为读者提供对该领域现状的全面了解,并为未来的研究做出贡献。
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