Catalyst-free
and mild synthetic methods for the construction of
hindered α-amino acid derivatives are presented herein. A wide
range of hindered amino acid amides can be readily obtained from the
reaction of α-halohydroxamates with a variety of amines, including
anilines, primary amines, and secondary amines. Moreover, the aza/aza-[4+3]
cycloaddition of in situ-generated aza-oxyallyl cations with 2-aminophenyl
α,β-unsaturated carbonyls to furnish seven-membered benzodiazepin-3-ones
is reported for the first time.
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