Constructing N-Acyl/N-Sulfonyl Aza-Sulfur Derivatives from Amides/Sulfonamides and Thiophthalimides via Oxidant Regulation

Here, we have constructed five distinct types of N-acyl or N-sulfonyl aza-sulfur scaffoldsusing readilyavailable (sulfon)amides and thiophthalimides with precise regulationof oxidants. Our novel methods feature one-pot mild reaction conditionsand simple operation, thereby making them highly convenient for thelate-stage diversification of various amide drugs, bioactive molecules,and peptides.

Automated summary

We have developed a method to construct five different types of N-acyl or N-sulfonyl aza-sulfur scaffolds using easily available (sulfon)amides and thiophthalimides. Our approach allows precise regulation of oxidants and features mild reaction conditions and simple operation, making it highly convenient for the late-stage diversification of various amide drugs, bioactive molecules, and peptides.