Highly Efficient Coupling of beta-Substituted Aminoethane Sulfonyl Azides with Thio Acids,toward a New Chemical Ligation Reaction

摘要

A highly efficient coupling of protected beta-substituted aminoethane sulfonyl azides with thio acids is reported.In the case of peptide thio acids,this method encompasses a new chemoselective ligation method.Furthermore,the resulting alpha-amino acyl sulfonamides can be alkylated with suitable electrophiles to obtain densely functionalized sulfonamide scaffolds.