Department of Chemistry, National Tsing Hua University, Hsinchu, Taiwan, R.O.C.
Angew Chem Int Ed Engl. 2019 Mar 18;58(12):3838-3842. doi: 10.1002/anie.201813315. Epub 2019 Feb 18.
The first successful example of the three-component coupling of N-alkylanilines, terminal alkynes, and alcohols was achieved at room temperature by a visible-light-mediated copper-catalyzed photoredox hydrogen-atom transfer process. This method allows preparation of propargylamines through uniquely selective α-C-H bond activation of unactivated alkylalcohols. Preliminary studies indicate that formation of α-oxy radical is operative. This approach facilitates rapid access to biologically important propargylamines from methanol as an abundant feedstock.
首例 N-烷基苯胺、末端炔烃和醇的三组分偶联反应在室温下通过可见光介导的铜催化光还原氢原子转移过程成功实现。该方法通过独特的选择性未活化的烷基醇的α-C-H 键活化来制备炔丙基胺。初步研究表明α-氧自由基的形成是可行的。这种方法有利于从甲醇这种丰富的原料快速获得具有生物重要性的炔丙基胺。
