Design And Synthesis Of Peptides With Monodisperse Polyethylene Glycol

Novel biomaterials for imaging capability is of great significance for the development of image-guided drug delivery and personalized therapy.Polyethylene glycol?PEG?has a wide range of applications in drug modification and drug delivery for its excellent biocompatibility and physicochemical properties.However,conventional polyethylene glycol is a complex mixture originated from polymerization and it brings many problems to drug development and drug delivery due to its polydispersity.In addition,it is very difficult to provide PEG with multi-functionality.Monodisperse PEG-based materials can solve these problems of polydispersity and multi-functionality.To this end,we synthesized a series of functional peptides by monodisperse PEG-based amino acid.These peptides has the properties of ¹⁹F magnetic resonance imaging(¹⁹F MRI)through introduce fluorine-containing groups into functionalized side chain provides a new imaging-traceable carrier for drug delivery.This paper is divided into the following sections:firstly,with macrocyclic sulfates as the key intermediates,a series of oligoethylene glycol?OEG?containing omega-amino acids were prepared with high efficiency.Secondly,lysine derivative with a fluorinated side chain was prepared with high efficiency.Thirdly,through Fmoc-based solid phase peptide synthesis,a series of novel ¹⁹F MRI-traceable biomaterials with monodisperse oligoethylene glycol?OEG?containing omega-amino acids and fluorinated lysine as backbone were prepared.