期刊
CHEMICAL COMMUNICATIONS
卷 49, 期 86, 页码 10175-10177出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3cc45118f
关键词
-
资金
- National Natural Science Foundation of China [21232006]
- National Basic Research Program of China [2009CB825300]
We report herein a CuBr-catalyzed three-component coupling of 2-methylbut-3-yn-2-ol, aldehydes and pyrrolidine or 1,2,3,4-tetra-hydroisoquinoline leading to the corresponding chiral propargylamines in excellent enantiomeric excess (91 to >99% ee) and high yields (79-95% yield). The dimethylcarbinol unit in 2-methylbut-3-yn-2-ol, which may be easily removed at the later stage to regenerate a terminal alkyne unit for further elaboration, plays a very important role in ensuring high enantioselectivity. This protocol provides easy and very general access to different terminal and non-terminal tertiary propargylic amines.
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