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Updated: Dec 13, 2025

The Synthesis, Characterization and Reactivity of a Series of Ruthenium N-triphosPh Complexes
Published on: April 10, 2015
Synthesis of PEG-Functionalized Amines Using Ruthenium-Catalyzed Hydrogen Borrowing
Federico V Rossi1, Jeremy T Starr2, Daniel P Uccello2
1School of Science and Technology, Chemistry Division, University of Camerino, via S. Agostino 1, I-62032 Camerino, MC, Italy.
We developed a new method for PEGylation of amines using hydrogen borrowing reductive amination. This efficient process yields PEGylated amines, including the drug quetiapine.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Catalysis
Background:
- Polyethylene glycol (PEG) is crucial in medicinal chemistry.
- PEGylation enhances drug properties.
- Efficient PEGylation of amines is needed.
Purpose of the Study:
- To describe a novel method for PEGylation of amines.
- To utilize hydrogen borrowing reductive amination for PEGylation.
- To demonstrate the synthesis of PEGylated amines and a drug molecule.
Main Methods:
- Employing [Ru(p-cymene)Cl2]2 catalyst.
- Using phosphorus-containing ligands (dppf or DPE).
- Utilizing hydrogen borrowing reductive amination for amine functionalization.
Main Results:
- Successful PEGylation of primary and secondary amines.
- Variety of PEGylated amine products obtained.
- Synthesis of quetiapine (Seroquel) in 62% isolated yield.
Conclusions:
- The described method is effective for amine PEGylation.
- This approach offers a viable route to PEGylated compounds.
- The method is applicable to pharmaceutical synthesis.
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