Department of Industrial and Engineering Chemistry, Institute of Chemical Technology, Indian oil Odisha Campus, IIT Kharagpur extension Centre, Mouza Samantpuri, Bhubaneswar, 751013, Odisha, India.
Department of Chemistry, National Institute of Technology Puducherry, Karaikal, 609609, Union Territory Puducherry, India.
Chem Asian J. 2022 Sep 14;17(18):e202200485. doi: 10.1002/asia.202200485. Epub 2022 Aug 10.
C -selective deuteration of aromatic aldehydes is of great importance for isotopic labeling and for improving the characteristics of drug molecules. Due to the recent increase in the use of deuterated pharmacological drugs, there is a pressing need for synthetic procedures that are efficient to produce deuterated aromatic aldehyde analouges. Deuterium labeling approaches are typically used as an effective tool for researching pharmaceutical absorption, distribution, metabolism, and excretion (ADME). Furthermore, deuterium-labeled pharmaceuticals are intended to increase therapeutic effectiveness and reduce side effects by extending the half-life of drug response. In the last few years, several catalytic or non-catalytic methods have been developed to synthesize deuterated aromatic aldehydes. In this concern, we offer a brief overview of the various synthetic strategies and practical methods for the formyl-selective deuterium labeling of aromatic aldehydes using different deuterium sources.
芳香醛的 C-选择性氘化对于同位素标记和改善药物分子的特性非常重要。由于氘化药物的使用最近有所增加，因此迫切需要高效的合成方法来生产氘代芳香醛类似物。氘标记方法通常被用作研究药物吸收、分布、代谢和排泄（ADME）的有效工具。此外，通过延长药物反应的半衰期，氘标记药物旨在提高治疗效果并减少副作用。在过去的几年中，已经开发了几种催化或非催化方法来合成氘代芳香醛。在这方面，我们简要概述了使用不同氘源对芳香醛进行甲酰基选择性氘标记的各种合成策略和实用方法。
