A Facile One-Pot Process for the Formation of Hindered Tertiary Amines

Molecules

Zhouyu Wang¹  Dong Pei¹  Yu Zhang¹  Chao Wang¹ 

[1] ¹Department of Pharmaceutics Engineering, Xihua University, Chengdu 610039, China ²Natural Products Research Center, Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, China

关键词: reductive amination;    tertiary amine;    Lewis base;    trichlorosilane;    ketone;   

DOI  :  10.3390/molecules17055151

来源: mdpi

【 摘 要 】

A simple and convenient method was developed for the preparation of hindered tertiary amines via direct reductive amination of ketones with secondary aryl amines, using trichlorosilane as reducing agent and tetramethylethylenediamine (TMEDA) as organic Lewis base activator. A broad range of ketones were reacted with N-methylaniline to afford the corresponding tertiary amine products in high yield. An open transition model was proposed for the reductive step.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.