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

A scalable and efficient approach for the synthesis of high-fidelity PEG(n)-NH(2)s has been developed. In this process, (Boc)(2)NH 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)-NH(2)s with different functional groups or topological structures are synthesized to demonstrate the versatility of this novel method. Additionally, mPEG(114)-NH2 can be converted to mPEG(114)-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.