Department of Chemistry, Imperial College London, Molecular Sciences Research Hub, W12 0BZ, London, UK.
Massachusetts Institute of Technology, Department of Chemistry, 77, Massachusetts Avenue, Cambridge, MA 02139-4307, USA.
Org Biomol Chem. 2021 Jan 28;19(3):498-513. doi: 10.1039/d0ob02098b.
Due to the importance of the amino ketone motif in synthetic and medicinal chemistry, the number of protocols developed in recent years has considerably increased. This review serves to collate and critically evaluate novel methodologies published since 2011 towards this high value synthon. The chapters are divided by the requisite functionality in the starting material, and an emphasis is placed on discussing functional group compatibility and resultant product substitution patterns. Throughout, applications to medicinal targets are highlighted and mechanistic details are presented, and we further provide a short outlook for future development and emerging potential within this area.
由于氨基酸酮基在合成和药物化学中的重要性，近年来开发的方法数量显著增加。本文综述了自 2011 年以来针对这一高价值合成子的新方法学，对其进行了收集和批判性评价。各章节按起始原料所需的功能进行划分，并重点讨论了官能团兼容性和所得产物的取代模式。全文突出了在药物靶点方面的应用，并介绍了反应机理的细节，进一步对该领域未来的发展和新兴潜力进行了简要展望。
