Late-Stage Functionalization for the Construction ­of Proline Skeleton in Peptides

Key words

late-stage functionalization - metal-free C–H functionalization - visible-light-mediated reaction - skeleton editing

Significance

Late-stage, site-specific modification of peptides is one of the most important tools to access synthetically modified peptides. Recently, modification of peptides by C–H functionalization gained attention in peptide chemistry. In this present study, transition-metal-free and visible-light-promoted C–H functionalization for the construction of proline skeleton in peptides is described.

Comment

Visible-light-promoted selective editing of peptide skeleton via C–N bond formation at N-terminal aliphatic side chains proceeded smoothly to offer a series of proline skeletons in peptides. This reaction is highly selective and showcases broad substrate scope.

Publication History

Article published online:
17 January 2023