Regioselective liquid phase pegylation
AssigneeAres Trading S.A.
InventorsGilles Piquet, Luca Barbero, Silvio Traversa, Monica Gatti
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Abstract
A method is described for a method for the regioselective liquid-phase pegylation of GRF, which increases the yield of the GRF-PEG conjugate having 1 PEG molecule covalently bound to the e-amino group of Lys12. This method is characterized in that the reaction is carried out in a structuring solvent, such as trifluorethanol.
Claims5
A method for the liquid-phase regioselective synthesis of the GRF-PEG conjugate having one PEG unit covalently bound to the ε amino group of Lys12, characterized in that the conjugation reaction between the GRF peptide and the activated PEG is carried out in a structuring solvent.
The method according to anyone of the preceding claims, wherein the activated PEG is an alkylating or acylating PEG in its mono-methoxylated form.
The method according to any of the preceding claims, in which the structuring solvent is trifluoroethanol.
The method according to any of the preceding claims, in which the conjugation reaction is carried out at room temperature.
Dependencies are inferred from the claim text.