Center for Catalysis, Aarhus University, 8000 Aarhus C, Denmark.
Org Lett. 2011 Jan 21;13(2):328-31. doi: 10.1021/ol102812c. Epub 2010 Dec 17.
A convenient, efficient synthesis of 1,2,4-triazolines from α-isocyano esters/amides and azodicarboxylates is presented. The developed reaction cascade is based on a base-catalyzed hydrazination-type reaction followed by a subsequent cyclization providing the triazolines in good to excellent yields (75-99%). Phosphine-catalyzed and preliminary asymmetric phase-transfer catalysis approaches have also been investigated.
本文报道了一种方便、高效的 1,2,4-三唑啉的合成方法，该方法由α-异氰酸酯/酰胺和偶氮二甲酸酯反应得到。所开发的反应级联反应基于碱催化的腙化反应，随后进行环化反应，以良好至优秀的收率（75-99%）得到三唑啉。本文还研究了膦催化和初步的不对称相转移催化方法。
