4.8 Article

Efficient Microwave-Assisted One Shot Synthesis of Peptaibols Using Inexpensive Coupling Reagents

Journal

ORGANIC LETTERS
Volume 16, Issue 6, Pages 1783-1785

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol5003253

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Funding

  1. la Ligue Nationale Contre le Cancer
  2. Bonus Qualite Recherche of Perpignan University

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A diisopropylcarbodiimide/Oxyma (ethyl 2-cyano-2-(hydroxyimino)acetate) coupling cocktail was successfully incorporated into the automated microwave-assisted synthesis of two peptaibols and one analog, whose previously reported syntheses were complicated by steric hindrance. This method utilizes commercially available reagents and affords alamethicin F50/5 and bergofungin D in high yields and purities along with an appreciable reduction of synthesis time and cost. when compared to previously reported methods.

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