4.6 Article

Enantioselective synthesis of cyclic quaternary α-amino acid derivatives by chiral phosphoric acid catalysis

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ORGANIC & BIOMOLECULAR CHEMISTRY
卷 15, 期 28, 页码 6033-6041

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c7ob01149k

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  1. National Natural Science Foundation of China [21572200]
  2. Fundamental Research Funds for the Central Universities [2017QNA3013]

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A highly enantioselective aza-Friedel-Crafts reaction of N-sulfonyl cyclic ketimines with indoles catalyzed by chiral phosphoric acids has been developed. This methodology provides an efficient and facile route to indole-containing chiral cyclic alpha-amino acid derivatives bearing a quaternary stereocenter in high yields and up to 98% enantioselectivity.

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