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引用次数: 5
摘要
n -芳基环胺在有机溶剂中臭氧氧化得到n -芳基内酰胺。特别是，制备Xa因子抑制剂的关键中间体4-(4-氨基苯基)-morpolin-3-one的产率相当高。该方法代表了叔n芳基底物内酰胺化的另一种方法，并且基于在杂环中“无金属”地引入羰基功能。
N-aryl lactams by regioselective ozonation of N-aryl cyclic amines.
Ozonation of N-aryl-cyclic amines in organic solvents gave N-aryl-lactams regioselectively. In particular, 4-(4-aminophenyl)-morpolin-3-one, a key intermediate in the preparation of factor Xa inhibitors, was obtained in fair yields. The method represents an alternative approach for the lactamization of tertiary N-arylic substrates and is based on a "metal-free" introduction of the carbonyl function into the heterocyclic ring.
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