4.8 Article

Pyrrolidines and Piperidines by Ligand-Enabled Aza-Heck Cyclizations and Cascades of N-(Pentafluorobenzoyloxy)carbamates

Journal

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 57, Issue 18, Pages 5124-5128

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201801109

Keywords

aza-Heck reaction; cascade reactions; N-heterocycles; palladium

Funding

  1. EPSRC [EP/M506473/1]
  2. FAPESP [2016/00422-0]
  3. AstraZeneca
  4. Biotechnology and Biological Sciences Research Council [BB/F011539/1] Funding Source: researchfish
  5. Engineering and Physical Sciences Research Council [EP/K03927X/1, 1627995, EP/L011999/1] Funding Source: researchfish
  6. BBSRC [BB/F011539/1] Funding Source: UKRI
  7. EPSRC [EP/L011999/1, EP/K03927X/1] Funding Source: UKRI

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Ligand-enabled aza-Heck cyclizations and cascades of N-(pentafluorobenzoyloxy)carbamates are described. These studies encompass the first examples of efficient non-biased 6-exo aza-Heck cyclizations. The methodology provides direct and flexible access to carbamate protected pyrrolidines and piperidines.

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