We have developed a one-pot synthetic method for producing
1,2-diamines
from easily prepared and commercially available precursors through
a formal umpolung process. Our method utilizes an efficient [3 + 2]
cycloaddition as the key step in forming substituted 1,2-diamines
in moderate to high yields. These resulting compounds can undergo
subsequent transformations, demonstrating their utility as synthetic
building blocks for more complex scaffolds. Finally, we propose a
reasonable mechanism for this transformation using density functional
theory modeling, justifying the experimental observations.