Journal
TETRAHEDRON LETTERS
Volume 58, Issue 3, Pages 213-217Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2016.12.012
Keywords
Organocatalysis; Aza-Friedel-Crafts alkylation; Enantioselective; Indoles; alpha-Ketimino esters
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Funding
- Youth Innovation Promotion Association of the Chinese Academy of Sciences [2016318]
- National Natural Science Foundation of China [201101062]
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A highly enantioselective aza-Friedel-Crafts alkylation of indoles with cyclic aryl alpha-ketimino esters catalyzed by a chiral phosphoric acid has been developed, the corresponding alpha,alpha-disubstituted unnatural alpha-amino ester derivatives were obtained in moderate to high yields (67-85%) with high enantioselectivities (up to 93% ee) under mild reaction conditions. (C) 2016 Published by Elsevier Ltd.
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