A scalable and efficient approach to high-fidelity amine functionalized poly(ethylene glycol) derivatives

Abstract

A scalable and efficient approach for the synthesis of high-fidelity PEG_n-NH₂s has been developed. In this process, (Boc)₂NH is employed as an amination reagent to ensure the high efficiency of the reaction and the high-fidelity of the end-groups. A series of high-fidelity PEG_n-NH₂s with different functional groups or topological structures are synthesized to demonstrate the versatility of this novel method. Additionally, mPEG₁₁₄-NH₂ can be converted to mPEG₁₁₄-Mal quantitatively, which can efficiently couple with GSH, laying a foundation for the synthesis of high-quality drugs and development of novel therapeutics in a facile way.