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3 and the lithium amide is very important. A good yield of 1 a is obtained only if a ratio of 1:2 is chosen, cf. refs. [24-26].
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The palladium catalyzed amination is significantly more convenient than alternative routes based on the amination of aryne intermediates or on the alkylation of Schiff bases. For the latter methods see: A. R. Johnson, C. C. Cummins, Inorg. Synth. 1998, 32, 123-132.
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Bis(tert-butyl)(2-phenylphenyl)phosphine affords similar results (82%), whereas the use of BINAP instead of 5 delivers only 47% of amine 7a.
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3 groups of 11 constitute the only source of fluoride in this reaction. This indicates that the intermediates primarily formed are able to activate C-F bonds. This aspect is subject of further investigations in this laboratory and details will be reported in a forthcoming publication.
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