期刊
ORGANIC LETTERS
卷 13, 期 4, 页码 596-599出版社
AMER CHEMICAL SOC
DOI: 10.1021/ol102804p
关键词
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资金
- National Natural Science Foundation of China [20732003, 21021001]
- National Basic Research Program of China (973 Program) [2010CB833300]
The asymmetric alpha-amination of 4-substituted pyrazolones with azodicarboxylates was investigated for the first time, employing an N,N'-dioxide gadolinium(III) complex as the catalyst. The novel transformations exhibited high yield, and 4-amino-5-pyrazolone derivatives bearing a chiral quaternary center were obtained in excellent yields (up to 99%) and enantioselectivities (90%-97% ee) for a broad scope of 5-pyrazolones by using 1 mol A or only 0.05 mol % of catalyst.
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