jo500644v_si_002.cif (794.15 kB)

Catalytic Asymmetric Aza-ene Reaction of 3‑Indolylmethanols with Cyclic Enaminones: Enantioselective Approach to C3-Functionalized Indoles

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posted on 16.05.2014, 00:00 by Wei Tan, Bai-Xiang Du, Xin Li, Xu Zhu, Feng Shi, Shu-Jiang Tu
The catalytic asymmetric aza-ene reactions of 3-indolylmethanols with cyclic enaminones and the highly enantioselective aza-ene reactions utilizing cyclic aza-ene components have been established, which directly assemble isatin-derived 3-indolylmethanols and dimedone-derived enaminones into C3-functionalized chiral indoles with one all-carbon quaternary stereogenic center in high yields and excellent enantioselectivities (up to 99% yield, up to 95:5 er).