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Synthesis of 3-amino-3,4-dihydro-1H-quinolin-2-ones through regioselective palladium-catalyzed intramolecular cyclization.

  • April 6, 2016

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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