• Development of potent cholinesterase inhibitors based on a marine pharmacophore 

      Elumalai, Vijayaragavan; Trobec, Tomaz; Grundner, Maja; Labriere, Christophe; Frangez, Robert; Sepcic, Kristina; Hansen, Jørn H; Svensson, Johan (Journal article; Tidsskriftartikkel; Peer reviewed, 2022-07-01)
      The management of neurological disorders such as dementia associated with Alzheimer's or Parkinson's disease includes the use of cholinesterase inhibitors. These compounds can slow down the progression of these diseases and can also be used in the treatment of glaucoma and myasthenia gravis. The majority of the cholinesterase inhibitors used in the clinic are derived from natural products and our ...
    • A Green, Scalable, and Catalyst-Free One-Minute Synthesis of Quinoxalines 

      Elumalai, Vijayaragavan; Hansen, Jørn H (Journal article; Tidsskriftartikkel; Peer reviewed, 2021-02-10)
      A highly efficient and catalyst-free protocol is reported for the synthesis of quinoxalines via the classical cyclocondensation reaction between aryldiamines and dicarbonyl compounds. Remarkably simple and green reaction conditions employing methanol as solvent afforded medium to excellent yield of quinoxalines after only one-minute reaction time at ambient temperature. The conditions allow at least ...
    • A Green, Scalable, One-Minute Synthesis of Benzimidazoles 

      Elumalai, Vijayaragavan; Hansen, Jørn H (Journal article; Tidsskriftartikkel; Peer reviewed, 2020-01-24)
      Herein is reported a substantially improved synthesis of 2-substituted benzimidazoles by condensation of 1,2-diaminoarenes and aldehydes using methanol as the reaction medium. The developed method afforded moderate to excellent yields (33-96%) at ambient temperature, displays high functional group tolerance, is conducted open to air, and requires only one-minute reaction time under catalyst- ...
    • Microwave‐Assisted Synthesis of Heterocycles from Aryldiazoacetates 

      Kristoffersen, Tone; Elumalai, Vijayaragavan; Starck, Eliot; Cousin, Étienne; Hansen, Stephanie Ramona; Hansen, Jørn H (Journal article; Tidsskriftartikkel; Peer reviewed, 2020-11-17)
      Herein, we describe a rapid microwave-assisted, metal-free synthesis of substituted quinoxalinones and quinoxalines using the carbene-mediated reaction between aryldiazo esters and 1,2-diamines. The reaction can encompass a range of substituents and structural variations to afford quinoxalin-2-ones in 14–80 % yield and corresponding quinoxalines in good to excellent yields upon oxidation (67–96 %). ...
    • Phidianidine A and Synthetic Analogues as Naturally Inspired Marine Antifoulants 

      Labriere, Christophe; Elumalai, Vijayaragavan; Staffansson, Jannie; Cervin, Gunnar; Le Norcy, Tiffany; Denardou, Hugo; Réhel, Karine; Moodie, Lindon W. K.; Hellio, Claire; Pavia, Henrik; Hansen, Jørn H; Svenson, Johan (Journal article; Tidsskriftartikkel; Peer reviewed, 2020-10-15)
      Stationary and slow-moving marine organisms regularly employ a natural product chemical defense to prevent being colonized by marine micro- and macroorganisms. While these natural antifoulants can be structurally diverse, they often display highly conserved chemistries and physicochemical properties, suggesting a natural marine antifouling pharmacophore. In our current report, we investigate the ...
    • A scalable and green one-minute synthesis of substituted phenols 

      Elumalai, Vijayaragavan; Hansen, Jørn H (Journal article; Tidsskriftartikkel; Peer reviewed, 2020-11-07)
      A mild, green and highly efficient protocol was developed for the synthesis of substituted phenols via <i>ipso</i>-hydroxylation of arylboronic acids in ethanol. The method utilizes the combination of aqueous hydrogen peroxide as the oxidant and H<sub>2</sub>O<sub>2</sub>/HBr as the reagent under unprecedentedly simple and convenient conditions. A wide range of arylboronic acids were smoothly ...
    • Synthesis of 5,7-diarylindoles via Suzuki-Miyaura coupling in water 

      Elumalai, Vijayaragavan; Hansen, Jørn H (Journal article; Tidsskriftartikkel; Peer reviewed, 2021-11-16)
      The synthesis of novel 5,7-diaryl and diheteroaryl indoles has been explored via efficient double Suzuki–Miyaura coupling. The method notably employs a low catalyst loading of Pd(PPh<sub>3</sub>)<sub>4</sub> (1.5 mol%/coupling) and water as the reaction solvent to obtain 5,7-diarylated indoles without using N-protecting groups in up to 91% yield. The approach is also suitable for N-protected and ...