Journal
ORGANIC LETTERS
Volume 15, Issue 5, Pages 1060-1063Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol400064r
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- University of Antwerp (BOF)
- Fund for Scientific Research-Flanders (FWO-Flanders)
- Hercules Foundation
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An auto-tandem Pd-catalyzed process consisting of an intramolecular direct arylation and an intermolecular Buchwald-Hartwig reaction for C-ring amino-substituted 1-methyl-1H-alpha-carboline synthesis has been developed. A mechanistic study of the direct arylation reaction revealed a rate effect of the inorganic base on the C H activation step (base effect). The amines, reagents in the tandem protocol, appear to have a similar effect on the direct arylation.
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