Development of a solid-supported biotinylation reagent for efficient biotin labeling of SH groups on small molecules

We report here the design and synthesis of a novel and selective SH-group biotinylating reagent, KSH-1 (1), for the biotinylation of small molecules using solid phase chemistry. The results demonstrate that 1 efficiently biotinylated a small molecule, captopril, and afforded the product in high yield and purity.