A new method for post-assembly modification of peptides via the Pd-catalyzed endogenous group-directed sp^(3) C—H arylation with aryl iodides is developed.The sulfide side chain of methionine(Met)residue can facilita...A new method for post-assembly modification of peptides via the Pd-catalyzed endogenous group-directed sp^(3) C—H arylation with aryl iodides is developed.The sulfide side chain of methionine(Met)residue can facilitate the arylation of bothβandγmethyl C—H bonds of N-terminal aliphatic amino acids of peptides via formation of 5 or 6-membered palladacycle intermediates.The reactions can proceed in moderate to good yield and with excellent diastereoselectivity.展开更多
基金supported by the National Natural Science Foundation of China(21725204)Frontiers Science Center for New Organic Matter(63181206)Haihe Laboratory of Sustainable Chemical Transformations,and NCC2020FH02。
文摘A new method for post-assembly modification of peptides via the Pd-catalyzed endogenous group-directed sp^(3) C—H arylation with aryl iodides is developed.The sulfide side chain of methionine(Met)residue can facilitate the arylation of bothβandγmethyl C—H bonds of N-terminal aliphatic amino acids of peptides via formation of 5 or 6-membered palladacycle intermediates.The reactions can proceed in moderate to good yield and with excellent diastereoselectivity.
