Synthesis of 3-amino-3,4-dihydro-1H-quinolin-2-ones through regioselective palladium-catalyzed intramolecular cyclization
2016
Hallé, François | Van der Poorten, Olivier | Doebelin, Christelle | Niederst, Marie | Schneider, Séverine | Schmitt, Martine | Ballet, Steven | Bihel, Frédéric
In this Letter we explored the regioselective cyclization of 2-bromophenylalanine derivatives to access enantiopure dihydroquinolinones via an intramolecular regioselective Buchwald–Hartwig cyclization using Pd2(dba)3/XPhos as a catalytic system in the presence of BTPP as organic base. This procedure represents a promising strategy for the direct synthesis of bridged Phe-Xaa dipeptides.
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