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酰胺在生物活性化合物合成及修饰中的还原官能团化

Reductive Functionalization of Amides in Synthesis and for Modification of Bioactive Compounds.

作者信息

Czerwiński Paweł J, Furman Bartłomiej

机构信息

Institute of Organic Chemistry, Polish Academy of Sciences, Warsaw, Poland.

出版信息

Front Chem. 2021 Apr 26;9:655849. doi: 10.3389/fchem.2021.655849. eCollection 2021.

Abstract

In this review, applications of the amide reductive functionalization methodology for the synthesis and modification of bioactive compounds are covered. A brief summary of the different protocols is presented in the introduction, followed by the synthetic application of these in late-stage functionalization, leading to known pharmaceuticals or to their derivatives, including bioisosteres, with potential higher activity as the main axis of the article. The synthetic approach to natural products based on amide reduction is also discussed; however, this is given in a condensed form focusing on recent or as yet unexplored applications due to a number of recently published excellent reviews covering this topic. The aim of this review is to illustrate the potential of reductive functionalization of amides as an elegant and useful tool in the synthesis of bioactive compounds and inspire further work in this field.

摘要

本综述涵盖了酰胺还原官能团化方法在生物活性化合物合成与修饰中的应用。引言部分简要总结了不同的反应方案,随后介绍了这些方案在后期官能团化中的合成应用,以已知药物或其衍生物(包括生物电子等排体,且以具有潜在更高活性为主要内容)为导向。文中还讨论了基于酰胺还原的天然产物合成方法;然而,由于近期已发表了许多关于该主题的优秀综述,因此此处以浓缩形式呈现,重点关注近期或尚未探索的应用。本综述的目的是阐明酰胺还原官能团化作为生物活性化合物合成中一种优雅且有用的工具的潜力,并激发该领域的进一步研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1901/8107389/ed9635687edf/fchem-09-655849-g0001.jpg

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