252573-87-8Relevant articles and documents
2(1H)-Pyridone as Leaving Group in Acylation Reactions - Applications in Peptide Synthesis
Effenberger, Franz,Brodt, Werner
, p. 468 - 482 (2007/10/02)
Alkyl 2-pyridyl carbonates 3 or mixtures of 3 and the isomeric N-(alkoxycarbonyl)-2-pyridones 3' are useful for the introduction of urethane protective groups into amino acids.The N-protected amino acids 7 - 10 react with 2(1H)-pyridone (1a) using the carbodiimide method to yield 2-pyridyl active esters 11, which easily undergo coupling reactions with amino acid esters 12 with elimination of 1a to give peptides 13 in good yields as well as high optical purities.