Liao Jianhua, Tong Jinghui, Liu Liang, Ouyang Lu, Luo Renshi
School of Pharmaceutical Sciences, Gannan Medical University, Ganzhou 341000, China.
College of Chemistry and Environmental Engineering, Shaoguan University, Shaoguan 512005, China.
Molecules. 2024 May 30;29(11):2565. doi: 10.3390/molecules29112565.
-aryl-substituted pyrrolidines are important moieties widely found in bioactive substances and drugs. Herein, we present a practical reductive amination of diketones with anilines for the synthesis of -aryl-substituted pyrrolidines in good to excellent yields. In this process, the -aryl-substituted pyrrolidines were furnished via successive reductive amination of diketones via iridium-catalyzed transfer hydrogenation. The scale-up performance, water as a solvent, simple operation, as well as derivation of drug molecules showcased the potential application in organic synthesis.
芳基取代的吡咯烷是广泛存在于生物活性物质和药物中的重要部分。在此，我们报道了一种二酮与苯胺的实用还原胺化反应，用于合成芳基取代的吡咯烷，产率良好至优异。在这个过程中，芳基取代的吡咯烷是通过铱催化的转移氢化反应，经由二酮的连续还原胺化反应制得的。放大性能、以水为溶剂、操作简单以及药物分子的衍生化展示了其在有机合成中的潜在应用。
