Manganese‐Catalyzed Mono‐<i>N</i>‐Methylation of Aliphatic Primary Amines without the Requirement of External High‐Hydrogen Pressure
作者:Jiale Ji、Yinghao Huo、Zhaowen Dai、Zhening Chen、Tao Tu
DOI:10.1002/anie.202318763
日期:2024.3.22
A synergistic strategy enables the selective synthesis of mono-N-methylated aliphatic primary amines, including deuterium-labelled drugs. This innovative approach combines an earth-abundant manganese catalyst with a weak base, resulting in a practical and sustainable protocol for mono-N-methylation. By effectively inhibiting the formation of formamide byproducts, it eliminates the need for external
协同策略能够选择性合成单N-甲基化脂肪族伯胺,包括氘标记的药物。这种创新方法将地球上丰富的锰催化剂与弱碱相结合,形成了实用且可持续的单N-甲基化方案。通过有效抑制甲酰胺副产物的形成,无需外部高压氢气。