Organocatalytic Highly Enantioselective Monofluoroalkylation of 3-Bromooxindoles: Construction of Fluorinated 3,3鈥?Disubstituted Oxindoles and Their Derivatives
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- 作者：Chongyang Wu ; Guofeng Li ; Wangsheng Sun ; Ming Zhang ; Liang Hong ; Rui Wang
- 刊名：Organic Letters
- 出版年：2014
- 出版时间：April 4, 2014
- 年：2014
- 卷：16
- 期：7
- 页码：1960-1963
- 全文大小：307K
- 年卷期：v.16,no.7(April 4, 2014)
- ISSN：1523-7052
文摘
A new practical organocatalytic asymmetric protocol for the introduction of a monofluoroalkyl group into the oxindole framework has been successfully developed. Excellent diastereoselectivities (>20:1 dr) and enantioselectivities (93鈥?9% ee) of the products were obtained with a wide range of pre-electrophiles (3-bromooxindoles) and prenucleophiles (伪-fluorinated 尾-keto gem-diols). The obtained products themselves and their derivatives may significantly benefit drug discovery.