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Self-Catalyzed Rapid Synthesis Of N-Acylated/N-Formylated Alpha-Aminoketones And N-Hydroxymethylated Formamides From 3-Aryl-2h-Azirines And 2-Me/Ph-3-Aryl-2h-Azirines

ORGANIC LETTERS(2020)

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摘要
A rapid and effective method has been established for the synthesis of N-acylated alpha-aminoketone derivatives by the reaction of 3-aryl-2H-azirines and highly substituted 2-Me/Ph-3-aryl-2H-azirines with various carboxylic acids under ambient air within 10 min at room temperature. N-Trifluoroacetylated alpha-aminoketones with different substituents have been reported in the presence of trifluoroacetic acid. This protocol is equally effective to synthesize N-formylated alpha-aminoketone and N-hydroxymethylated formamide derivatives.
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