Key Laboratory of Synthetic and Nature Molecule Chemistry of Ministry of Education, Department of Chemistry & Materials Science , Northwest University , Xi'an 710127 , P. R. China.
Org Lett. 2018 Jun 1;20(11):3337-3340. doi: 10.1021/acs.orglett.8b01240. Epub 2018 May 23.
A novel and efficient strategy for the synthesis of 1,6-dihydropyridazines via copper-promoted 6- endo-trig cyclization of readily available β,γ-unsaturated hydrazones have been developed. A series of 1,6-dihydropyridazines have been synthesized by this method with good yields, high functional group tolerance, and remarkable regioselectivity under mild conditions. Importantly, the 1,6-dihydropyridazines can be efficiently converted to biologically important pyridazines in the presence of NaOH.
一种新颖高效的合成 1,6-二氢哒嗪的策略是通过铜促进的β,γ-不饱和腙的 6-endo-trig 环化反应来实现的。通过这种方法，一系列的 1,6-二氢哒嗪可以在温和的条件下以良好的收率、高官能团容忍度和显著的区域选择性合成。重要的是，在存在 NaOH 的情况下，1,6-二氢哒嗪可以有效地转化为具有生物重要性的哒嗪。
