4.7 Article

Increasing synthetic efficiency via direct C-H functionalization: formal synthesis of an inhibitor of botulinum neurotoxin

Journal

CHEMICAL COMMUNICATIONS
Volume 47, Issue 16, Pages 4679-4681

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c1cc10755k

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Funding

  1. National Science Foundation [0847222]
  2. Rhode Island INBRE (NIH-NCRR) [P20RR016457]
  3. NATIONAL CENTER FOR RESEARCH RESOURCES [P20RR016457] Funding Source: NIH RePORTER

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A new and efficient scheme for the synthesis of one of the best known inhibitors of botulinum neurotoxin serotype A (BoNTA) is reported herein. The synthetic route involves two palladium-catalyzed C-H functionalization reactions, formally activating three C-H bonds.

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