Department of Chemistry and Center for Sustainable Chemistry, Ghent University, 9000 Ghent, Belgium.
VITO (Flemish Institute for Technological Research), Separation and Conversion Technology, Boeretang 200, 2400 Mol, Belgium.
Molecules. 2022 Jun 2;27(11):3583. doi: 10.3390/molecules27113583.
α-Haloketones play an essential role in the synthesis of complex -, -, -heterocycles; of which some exhibit a remarkable biological activity. Research further illustrated that α-bromo-, α-chloro-, and α-iodoketones are key precursors for blockbuster pharmacological compounds. Over the past twenty years, substantial advances have been made in the synthesis of these industrially relevant building blocks. Efforts have focused on rendering the synthetic protocols greener, more effective and versatile. In this survey, we summarised and thoroughly evaluated the progress of the field, established in the past two decades, in terms of generality, efficacy and sustainability.
α-卤代酮在复杂的 -, -, -杂环的合成中起着至关重要的作用;其中一些具有显著的生物活性。研究进一步表明，α-溴代酮、α-氯代酮和α-碘代酮是重磅药物化合物的关键前体。在过去的二十年里，这些工业相关构建块的合成取得了重大进展。人们致力于使合成方案更加绿色、高效和多功能。在本综述中，我们总结和全面评估了过去二十年该领域的进展，从通用性、效率和可持续性方面进行了评价。
