Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, School of Pharmaceutical Sciences, and College of Chemistry and Molecular Engineering, Zhengzhou University , Zhengzhou, Henan 450001, P. R. China.
Org Lett. 2016 Jul 15;18(14):3390-3. doi: 10.1021/acs.orglett.6b01546. Epub 2016 Jul 1.
We present a metal-free [2 + 2 + 2] cycloaddition of ynamides with nitriles that enables highly efficient access to 2,4-diaminopyridines. This catalytic protocol is more environmentally friendly and allows for a concomitant construction of C-C and C-N bonds between ynamides and nitriles, exhibiting excellent chemoselectivity, regioselectivity, and wide functional groups tolerance.
我们提出了一种酰胺与腈的无金属[2 + 2 + 2]环加成反应，可高效构建 2,4-二氨基吡啶。该催化方法更为环保，且酰胺与腈之间可同时构建 C-C 和 C-N 键，具有优异的化学选择性、区域选择性和广泛的官能团耐受性。
