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A facile protocol for N-Cbz protection of amines in PEG-600
Authors:Chun Lin Zhang  Dong Feng Zhang  Hong Yi Zhao  Zi Yun Lin  Hai Hong Huang
Institution:Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China
Abstract:An efficient and eco-friendly protocol for the chemoselective N-benzyloxycarbonylation of amines was described. The reaction of amines with benzyl chloroformate (Cbz-Cl) in the presence of PEG-600 at room temperature afforded the corresponding N-Cbz derivatives in excellent yields. The method is applicable to the N-Cbz protection of aliphatic (acyclic and cyclic) and aromatic amines.
Keywords:Benzyl chloroformate (Cbz-Cl)  N-Cbz protection  Amines  PEG-600  
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