Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 76, Issue 8, Pages 2884-2887Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jo102022g
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Funding
- National Basic Research Program of China [2009CB626604, 2010CB833203]
- NSFC [20972058, 21032005]
- MOE of P. R. China
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The first asymmetric Michael addition of 1-acetylindolin-3-ones to beta-nitrostyrenes has been developed. 2-Substituted indolin-3-one derivatives were obtained with excellent yields (up to 99%) and good stereoselectivities (up to 28:1 dr and 92% ee), which could be transformed into 2-functionalized indoles easily without racemization. This achievement might further contribute to the chemistry and pharmacology of indole-related compounds.
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