Shenzhen Grubbs Institute, Department of Chemistry, and, Guangdong Provincial Key Laboratory of Catalysis, Southern University of Science and Technology, Shenzhen, 518055, Guangdong, P. R. China.
Angew Chem Int Ed Engl. 2021 Apr 26;60(18):9875-9880. doi: 10.1002/anie.202016679. Epub 2021 Mar 18.
Direct and selective synthesis of primary amines from easily available precursors is attractive yet challenging. Herein, we report the rapid synthesis of primary amines from alkenes via metal-free regioselective hydroamination at room temperature. Ammonium carbonate was used as ammonia surrogate for the first time, allowing for efficient conversion of terminal and internal alkenes into linear, α-branched, and α-tertiary primary amines under mild conditions. This method provides a straightforward and powerful approach to a wide spectrum of advanced, highly functionalized primary amines which are of particular interest in pharmaceutical chemistry and other areas.
直接和选择性地从易得前体制备伯胺具有吸引力,但也具有挑战性。在此,我们报道了在室温下通过无金属区域选择性氢胺化快速合成伯胺。首次使用碳酸铵作为氨源,可在温和条件下有效地将末端和内部烯烃转化为线性、α-支链和α-叔伯胺。该方法为广泛的先进的、高度官能化的伯胺提供了一种直接而强大的方法,这些伯胺在药物化学和其他领域具有特别的兴趣。