A simple
catalyst- and promoter-free protocol has been developed
for the transamidation of weakly nucleophilic aromatic amines with
formamide derivatives and low-reactivity tertiary amides with aliphatic
amines. This strategy is advantageous because no catalyst or promoters
are needed, no additives are required, separation and purification
is easy, and the reaction is scalable. Significantly, this strategy
was further applied to synthesize several pharmaceutical molecules
on a gram scale, and excellent yields were achieved.
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