Herein, the sulfonyl fluoro isocyanides
were first developed as
a new type of SuFExable synthon, and they are used as building blocks
in the Ugi reaction (U-4CR). The Ugi reaction was established and
the substrate scope was investigated, and various sulfonyl fluoro
α-amino amides and peptides could be reached in a one-step synthesis.
Therefore, this protocol opens a new vision for SuFExable building
blocks and click chemistry, and it also provides a distinct approach
to sulfonyl fluoro peptides.