2. Academic Validation
  3. Enantioselective Total Synthesis of (+)-Dihydro-β-erythroidine

Enantioselective Total Synthesis of (+)-Dihydro-β-erythroidine

  • J Am Chem Soc. 2019 Jun 5;141(22):8783-8786. doi: 10.1021/jacs.9b04626.
Sebastian Clementson 1 2,  Mikkel Jessing 2,  Henrik Pedersen 3,  Paulo Vital 2,  Jesper L Kristensen 1
Affiliations

Affiliations

  • 1 Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Universitetsparken 2 , 2100 Copenhagen , Denmark.
  • 2 Molecular Discovery and Innovation , H. Lundbeck A/S , Ottiliavej 9 , 2500 Valby , Denmark.
  • 3 Compound Management and Analytical Chemistry , H. Lundbeck A/S , Ottiliavej 9 , 2500 Valby , Denmark.
PMID: 31122014 DOI: 10.1021/jacs.9b04626
Abstract

Erythrina Alkaloids represent a rich source of complex polycyclic, bioactive Natural Products. In addition to their sedative and hypotensive effect, their curare-like activity and structural framework have made them attractive targets for synthetic and medicinal chemists. (+)-Dihydro-β-erythroidine (DHβE), the most potent nicotine acetylcholine receptor antagonist (nAChR) of the Erythrina family, is synthesized for the first time in 13 steps from commercially available material.

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