Chiral Phosphoric Acid Catalyzed Highly Enantioselective Friedel鈥揅rafts Alkylation Reaction of C3-Substituted Indoles to 尾,纬-Unsaturated 伪-Ketimino Esters
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- 作者：Bo Bi ; Qin-Xin Lou ; Yu-Yang Ding ; Sheng-Wei Chen ; Sha-Sha Zhang ; Wen-Hui Hu ; Jun-Ling Zhao
- 刊名：Organic Letters
- 出版年：2015
- 出版时间：February 6, 2015
- 年：2015
- 卷：17
- 期：3
- 页码：540-543
- 全文大小：309K
- ISSN：1523-7052
文摘
A highly enantioselective C2 Friedel鈥揅rafts alkylation reaction of 3-substituted indoles to 尾,纬-unsaturated 伪-ketimino esters has been developed. This reaction was efficiently catalyzed by a chiral phosphoric acid catalyst. The corresponding C2-substituted indole derivatives, bearing an 伪-ketimino ester motif, were obtained in moderate to high yields (up to 93%) and with high enantioselectivities (up to >99% ee).