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Advances in the Synthesis of Methylated Products through Indirect Approaches
Advanced Synthesis & Catalysis ( IF 4.4 ) Pub Date : 2019-11-14 , DOI: 10.1002/adsc.201901240
Yantao Chen 1
Affiliation  

Methylation is a well‐known structural modification in organic and medicinal chemistry. In addition to using conventional methylation reagents for direct methylation, indirect methylation approaches have been also successfully applied, particularly to tackle the isolation difficulty among the methylated product, the unreacted starting material, and the dimethylated by‐product due to the structural similarities between them. This review summarizes recent advances in the synthesis of methylated products through indirect approaches – transforming functionalized intermediates into the methylated products. The indirect methodologies surveyed in this review are useful for chemists to select appropriate methylation strategies, particularly for the challenging synthesis of methylated products at a large scale in drug discovery.

中文翻译:

间接合成甲基化产物的研究进展

甲基化是有机化学和药物化学中众所周知的结构修饰。除了使用常规的甲基化试剂进行直接甲基化以外,间接甲基化方法也已成功应用,特别是解决了由于甲基化产物,未反应的起始原料和二甲基化副产物之间的结构相似而导致的分离困难。这篇综述总结了通过间接方法将甲基化产物合成的最新进展,即将功能化的中间体转变为甲基化产物。本综述中调查的间接方法学对化学家选择合适的甲基化策略很有用,特别是在药物发现中大规模挑战性地合成甲基化产物方面。
更新日期:2019-11-14
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