A new, one-pot, regioselective preparation of 2,5,6,7-tetrahydroimidazo[1,2-a]imidazol-3-ones by a sequential aza-Wittig/nucleophilic addition/cyclization reaction was developed. The aza-Wittig reactions of ethyl (2Z)-3-aryl-2-[(triphenylphosphoranylidene)amino] acrylates with aryl isocyanates produced carbodiimide intermediates that were then treated sequentially with 2-aminoethanol and tosyl chloride/triethylamine
2,5,6,7-四氢
咪唑并[1,2-a]
咪唑-3-酮通过连续的氮杂-Wittig/亲核加成/环化反应,开发了一种新的单锅区域选择性制备方法。(2Z)-3-芳基-2-[(三苯基亚膦基)
氨基]
丙烯酸乙酯与异
氰酸芳基酯的氮杂-Wittig反应产生碳二
亚胺中间体,然后依次用2-
氨基
乙醇和甲
苯磺酰氯/
三乙胺处理,得到相应的(2Z) )-2-[(取代的)亚苄基]-2,5,6,7-四氢-3H-
咪唑并[1,2-a]
咪唑-3-酮以良好的总产率和高区域选择性。