Abstract
Carbonylimidazol-l-yl-mPEG is obtained quantitatively by reacting methoxypoly(ethyleneglycol) (mPEG) with 1.1 Eq of N,N′-carbonyldiimidazole in the presence of a stoechiometric amount of 4-dimethyl-aminopyridine used as hypernucleophilic acylation catalyst. Carbonylimidazol-l-yl-mPEG is quite stable in aqueous solutions with half-lives up to 70 h in pHs ranging from 6.0 to 7.0 at 25‡C. From reactivity studies toward amines with various nucleophilic strengths, it is suggested that carbonylimidazol-l-yl-mPEG may be best used to modify α-amino terminal function of proteins selectively or to introduce amino function on PEG chains.
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Brygier, J., Gelbcke, M., Guermant, C. et al. Covalent attachment of poly(ethyleneglycol) to peptides and proteins. Appl Biochem Biotechnol 42, 127–135 (1993). https://doi.org/10.1007/BF02788048
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DOI: https://doi.org/10.1007/BF02788048