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Keywords:

  • asymmetric synthesis;
  • cycloaddition;
  • heterocycles
Thumbnail image of graphical abstract

Break the cycle: The title reaction proceeds with a variety of alkyne substrates in good yield and high enantioselectivity. Upon reduction of the vinylogous amide in high diastereoselectivity (>19:1) and cleavage of the tether, N-methylpiperidine products with functional group handles can be accessed (see scheme).