三丁基碘化铵/过硫酸钾促进的烯酮缩醛、-缩硫酮与偕二氮杂苯的[4 + 2]环加成反应。
TBAI/KSO-Promoted [4 + 2] Annulation of Ketene ,-Acetals and -Tosylhydrazones toward Pyridazines.
机构信息
State Key Laboratory of Biobased Material and Green Papermaking, Qilu University of Technology, Shandong Academy of Sciences, Jinan 250353, P. R. China.
Advanced Research Institute for Multidisciplinary Science, Qilu University of Technology, Shandong Academy of Sciences, Jinan 250353, P. R. China.
出版信息
Org Lett. 2021 Mar 5;23(5):1606-1610. doi: 10.1021/acs.orglett.1c00026. Epub 2021 Feb 10.
A TBAI/KSO-promoted [4 + 2] annulation of ketene -acetals, and -tosylhydrazones was efficiently developed, enabling straightforward access to a variety of trisubstituted pyridazines in reasonable to good yields. The synthetic methodology features a broad substrate scope and a good functional group tolerance. Control experiments demonstrated the indispensability of the alkylthio functionality in the enaminone substrates.
TBAI/KSO 促进的酮烯醇缩醛和对甲苯磺酰腙的[4 + 2]环加成反应被高效开发，为各种三取代哒嗪的合成提供了一种直接、合理收率的方法。该合成方法具有广泛的底物范围和良好的官能团耐受性。控制实验表明在烯胺酮底物中烷硫基的不可或缺性。
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