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Enantioselective Synthesis of Substituted Piperidines by Addition of Aryl Grignard Reagents to Pyridine N-Oxides.

Author

  • Munawar Hussain
  • Thomas Sainte-Luce Banchelin
  • Hans Andersson
  • Roger Olsson
  • Fredrik Almqvist

Summary, in English

The synthesis of optically active piperidines by enantioselective addition of aryl Grignard reagents to pyridine N-oxides and lithium binolate followed by reduction is reported for the first time. The reaction results in high yields (51-94%) in combination with good ee (54-80%). Some of these products were subsequently recrystallized, affording enhanced optical purities (>99% ee).

Topic

  • Organic Chemistry

Status

Published

ISBN/ISSN/Other

  • ISSN: 1523-7052