| 冯波,滕大为,曹国锐.化学通报,2023,86(8):977-984. |
| α,β-不饱和酰胺的合成研究进展 |
| Progress in Synthesis of α,β-Unsaturated Amides |
| 投稿时间：2022-11-28 修订日期：2023-02-02 |
| DOI： |
| 中文关键词: α,β-不饱和酰胺 过渡金属催化 合成 |
| 英文关键词:α,β-unsaturated amides Transition-metal catalyze Synthesis. |
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| 中文摘要: |
| α,β-不饱和酰胺是有机合成中的重要基团，存在于某些蛋白质以及高分子化合物的骨架结构中，因其可以与特定蛋白质的独特半胱氨酸残基发生不可逆的异-迈克尔加成反应共价结合细胞靶标，被广泛应用于药物合成中，使得此类化合物的合成成为药物化学的研究热点。本文主要分为过渡金属催化和无过渡金属合成两大方面，包括铜催化、钯催化、钴催化、镍催化等过渡金属催化以及无过渡金属合成等部分，对近年来α,β-不饱和酰胺基团的合成方法进行总结与评述，并对部分反应机理进行了阐述。 |
| 英文摘要: |
| α,β-unsaturated amides are important groups in organic synthesis. They exist in the backbone structure of some proteins and polymers. They are widely used in drug synthesis because they can covalently bind to cellular targets through irreversible iso-Michael addition reaction with unique cysteine residues of specific proteins. Therefore, the synthesis of such compounds has become a research hotspot in medicinal chemistry. This paper mainly includes transition metal catalysis and transition metal-free synthesis, including transition metal catalysis, palladium catalysis, cobalt catalysis, nickel catalysis and transition metal-free synthesis. The synthesis methods of α,β-unsaturated amide groups in recent years are summarized and commented, and some reaction mechanisms are also described. |
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