Method for solid phase synthesis of liraglutide

摘要

A method for the solid phase synthesis of liraglutide, characterized in that the method comprises the following steps: A) in the presence of an activating agent system, Fmoc-Gly-resin is obtained by coupling glycine protected with Fmoc N- terminal (Fmoc-Gly-OH) to a solid phase resin support; B) by solid phase synthesis, amino acids with N-terminal Fmoc protection and side chain protection are sequentially coupled onto the liraglutide peptide backbone sequence, where Fmoc-Lys (Alloc) -OH is used for lysine; C) the Alloc protecting group for the lysine side chain is removed; D) by solid phase synthesis, palmitoyl-Glu-OtBu is coupled to the lysine side chain; E) crude liraglutide is obtained by cleavage and removal of the protecting groups and the resin; F) liraglutide is finally obtained by purification and lyophilization.