An asymmetric pericyclic cascade approach to 3-alkyl-3-aryloxindoles: generality, applications and mechanistic investigations.

نویسندگان

  • Edward Richmond
  • Kenneth B Ling
  • Nicolas Duguet
  • Lois B Manton
  • Nihan Çelebi-Ölçüm
  • Yu-Hong Lam
  • Sezen Alsancak
  • Alexandra M Z Slawin
  • K N Houk
  • Andrew D Smith
چکیده

The reaction of L-serine derived N-arylnitrones with alkylarylketenes generates asymmetric 3-alkyl-3-aryloxindoles in good to excellent yields (up to 93%) and excellent enantioselectivity (up to 98% ee) via a pericyclic cascade process. The optimization, scope and applications of this transformation are reported, alongside further synthetic and computational investigations. The preparation of the enantiomer of a Roche anti-cancer agent (RO4999200) 1 (96% ee) in three steps demonstrates the potential utility of this methodology.

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عنوان ژورنال:
  • Organic & biomolecular chemistry

دوره 13 6  شماره 

صفحات  -

تاریخ انتشار 2015