Recent Advances in Synthesis of Enantioenriched 2‐Substituted Piperidine Derivatives

IF 2.8 4区 化学 Q1 CHEMISTRY, ORGANIC Asian Journal of Organic Chemistry Pub Date : 2024-10-01 DOI:10.1002/ajoc.202400257
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Abstract

Enantioenriched 2‐substituted piperidines are very important unit for drug discovery. Ready access to a wide range of such compounds, decorated with functional handles at 2‐position with stereo‐defined centre significantly enhance the quality and diversity of chemical libraries for screening of drug discovery. The ability to control the stereochemistry of piperidine at the 2‐position remains an area of interest in organic synthesis to allow the development of novel, structurally diverse 3D molecules. Among the various ways to obtain enantioenriched 2‐substituted piperidines, asymmetric hydrogenation is widely studied. Asymmetric synthesis, Kinetic resolution, and chiral pool synthesis methodologies are also important ways to obtain the enantioenriched 2‐substituted piperidines. This review article summarized the main four ways to achieve particularly the enantioenriched substituted piperidines only at 2‐position considering the chemical routes, excluding the biocatalytic approach. 1. Introduction 2.1 Asymmetric Hydrogenation of 2‐substituted Pyridines 2.2 Asymmetric Synthesis 2.3. Kinetic resolution of racemic 2‐substituted Piperidine derivatives 2.4. Chiral pool synthesis 3. Conclusions & outlook
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对映体 2-取代哌啶衍生物合成的最新进展
对映富集的 2-取代哌啶是药物发现中非常重要的单元。通过在 2-位上装饰具有立体定义中心的官能团,可以随时获得范围广泛的此类化合物,这大大提高了用于药物发现筛选的化学文库的质量和多样性。控制哌啶 2 位立体化学的能力仍然是有机合成领域的一个关注点,它有助于开发结构多样的新型三维分子。在获得对映体丰富的 2-取代哌啶的各种方法中,不对称氢化法被广泛研究。不对称合成法、动力学解析法和手性池合成法也是获得对映体富集的 2-取代哌啶的重要方法。本综述文章总结了除生物催化方法外,仅从化学途径获得对映富集的 2 位取代哌啶的四种主要方法。
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来源期刊
CiteScore
4.70
自引率
3.70%
发文量
372
期刊介绍: Organic chemistry is the fundamental science that stands at the heart of chemistry, biology, and materials science. Research in these areas is vigorous and truly international, with three major regions making almost equal contributions: America, Europe and Asia. Asia now has its own top international organic chemistry journal—the Asian Journal of Organic Chemistry (AsianJOC) The AsianJOC is designed to be a top-ranked international research journal and publishes primary research as well as critical secondary information from authors across the world. The journal covers organic chemistry in its entirety. Authors and readers come from academia, the chemical industry, and government laboratories.
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