The first solid phase synthesis of 1,2,4-oxadiazolines via 1,3-dipolar cycloaddition of nitrile oxide generated in situ on solid support with a variety of imines is described. The synthetic sequences were performed in parallel one-pot fashion. Cleavage from the support under two different mild conditions afforded a library of 1,2,4-oxadiazolines in good yields and purity.
首次报道了通过固相支持上原位生成的亚
氨酸酯与各种
亚胺的1,3-偶极环加成反应合成
1,2,4-恶二唑啉的固相合成方法。合成序列采用并行的一锅法进行。在两种不同的温和条件下从固相支持上脱除,得到了产率高且纯度良好的
1,2,4-恶二唑啉化合物库。