From Industrial Method to the Use of Silylated P(III) Reagents for the Synthesis of Relevant Phosphonylated Molecules,Organic Process Research & Development

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From Industrial Method to the Use of Silylated P(III) Reagents for the Synthesis of Relevant Phosphonylated Molecules
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-01-23 , DOI: 10.1021/acs.oprd.9b00490
Jade Dussart ₁ , Julia Deschamp ₁ , Evelyne Migianu-Griffoni ₁ , Marc Lecouvey ₁

Affiliation

Phosphonates and their derivatives widely represent important pharmacophores in various classes of therapeutic agents from antivirals to antibiotics. Among these phosphonylated compounds, 1-hydroxymethylene-1,1-bisphosphonates (HMBPs) have occupied a very important place for 30 years now and are currently used in medicine for their inhibitory properties on bone resorption. HMBPs also exhibit direct and indirect antitumor effects in vitro against a broad variety of tumor cell lines, including melanoma, mesothelioma, prostate, breast, lung, and myeloma cancer cells. This review will discuss the various syntheses of bisphosphonates with the goal of illustrating their potential interest for the development of therapeutic agents. We will also disclose our latest achievements in phosphinate chemistry.

中文翻译：

从工业方法到使用甲硅烷基化的P（III）试剂合成相关的膦酰化分子

膦酸酯及其衍生物广泛地代表了从抗病毒药到抗生素的各种治疗剂中的重要药效团。在这些膦酰化的化合物中，1-羟基亚甲基-1,1-双膦酸酯（HMBPs）占据了非常重要的位置已有30年了，目前由于其对骨吸收的抑制作用而被用于医学领域。HMBP在体外还对多种肿瘤细胞系（包括黑素瘤，间皮瘤，前列腺癌，乳腺癌，肺癌和骨髓瘤癌细胞）表现出直接和间接的抗肿瘤作用。这篇综述将讨论双膦酸酯的各种合成，以说明其对治疗剂开发的潜在兴趣。我们还将披露在次膦酸酯化学方面的最新成就。

更新日期：2020-01-23

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