Journal
ADVANCED SYNTHESIS & CATALYSIS
Volume 360, Issue 10, Pages 2049-2054Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.201800181
Keywords
aza-Friedel-Crafts; asymmetric organo-catalysis; pyrazolinone ketimines; hydroxyindoles; electron-rich phenols
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Funding
- Fundamental Research Funds for the Central Universities
- National Natural Science Foundation of China [21572053]
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A variety of enantioenriched indole derivatives substituted in the benzene ring were synthesised via an organocatalytic asymmetric aza-Friedel-Crafts reaction of pyrazolinone ketimines with hydroxyindoles. This reaction was also applicabled to electron-rich phenols, yielding the desired products in high yields (up to 99%) and excellent stereo-selectivities (91-99% ee). Moreover, this method presents its potential in the synthesis of structurally novel indole-pyrazolinone conjugate derivatives.
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