Efficient and chemoselective alkylation of amines/amino acids using alcohols as alkylating reagents under mild conditions.
We report a mild and environmentally benign method for the synthesis of tertiary amines using alcohols as the alkylating reagents. Not only secondary amines such as piperazines but also amino acids and amino alcohols can be N-alkylated selectively. For N,O-benzyl protected amino alcohols, both N,O-de-benzylation and N-methylation were achieved in one-pot.
Xu
Chu-Pei
CP
Department of Chemistry and Key Laboratory for Chemical Biology of Fujian Province, College of Chemistry & Chemical Engineering, Xiamen University, Xiamen, Fujian 361005, China.
Xiao
Zhen-Hua
ZH
Zhuo
Bi-Qin
BQ
Wang
Yu-Huang
YH
Huang
Pei-Qiang
PQ
D000438:Alcohols / Q000737:chemistry*; D000477:Alkylating Agents / Q000737:chemistry*; D000478:Alkylation; D000588:Amines / Q000737:chemistry*; D000596:Amino Acids / Q000737:chemistry*; D055772:Green Chemistry Technology / Q000379:methods*; D013379:Substrate Specificity
D000438:Alcohols; D000477:Alkylating Agents; D000588:Amines; D000596:Amino Acids