Unnatural amino acids(UAAs)have broad applications in pharmaceutical sciences and biological studies.Current synthetic methods for UAAs mainly rely on asymmetric catalysis and often require several steps.There is a la...Unnatural amino acids(UAAs)have broad applications in pharmaceutical sciences and biological studies.Current synthetic methods for UAAs mainly rely on asymmetric catalysis and often require several steps.There is a lack of direct and simple methods.To address this challenge,we designed the LADA(labeling-activation-desulfurization-addition)strategy:selective labeling and activation of cysteine residues,the photocatalytic desulfurization and the subsequent radical addition to alkenes.Although composed of two steps,it is one-pot synthesis and has advantages such as high functional group tolerance,biocompatible reaction condition,and retained stereochemistry.This highly efficient strategy was successfully applied in the direct synthesis of unnatural amino acids and modifications of peptides with more than 50 examples.展开更多
A visible-light-induced metal-free desulfurization method for thiols and disulfides has been explored.This radical desulfurization features mild conditions,robustness,and excellent functionality compatibility.It was s...A visible-light-induced metal-free desulfurization method for thiols and disulfides has been explored.This radical desulfurization features mild conditions,robustness,and excellent functionality compatibility.It was successfully applied not only to the desulfurization of small molecules,but also to peptides.展开更多
文摘Unnatural amino acids(UAAs)have broad applications in pharmaceutical sciences and biological studies.Current synthetic methods for UAAs mainly rely on asymmetric catalysis and often require several steps.There is a lack of direct and simple methods.To address this challenge,we designed the LADA(labeling-activation-desulfurization-addition)strategy:selective labeling and activation of cysteine residues,the photocatalytic desulfurization and the subsequent radical addition to alkenes.Although composed of two steps,it is one-pot synthesis and has advantages such as high functional group tolerance,biocompatible reaction condition,and retained stereochemistry.This highly efficient strategy was successfully applied in the direct synthesis of unnatural amino acids and modifications of peptides with more than 50 examples.
基金We thank Shanghai Jiao Tong University and the National"1000-Youth Talents Plan"for financial support.
文摘A visible-light-induced metal-free desulfurization method for thiols and disulfides has been explored.This radical desulfurization features mild conditions,robustness,and excellent functionality compatibility.It was successfully applied not only to the desulfurization of small molecules,but also to peptides.
