2. Academic Validation
  3. Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity

Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity

  • Bioorg Med Chem. 2016 Nov 1;24(21):5115-5126. doi: 10.1016/j.bmc.2016.08.029.
Aws M Hamdy 1,  Zien Khaddour 2,  Najim A Al-Masoudi 3,  Qamar Rahman 4,  Christian Hering-Junghans 2,  Alexander Villinger 2,  Peter Langer 5
Affiliations

Affiliations

  • 1 Institute für Chemie, Universitat Rostock, Albert Einstein Str. 3a, 18059 Rostock, Germany; Department of Chemistry, College of Science, University of Mosul, Mosul, Iraq.
  • 2 Institute für Chemie, Universitat Rostock, Albert Einstein Str. 3a, 18059 Rostock, Germany.
  • 3 Department of Chemistry, College of Science, University of Basrah, Basrah, Iraq.
  • 4 Institute für Chemie, Universitat Rostock, Albert Einstein Str. 3a, 18059 Rostock, Germany; Amity University, Lucknow Campus, Viraj Khand-5, Gomti Nagar, Lucknow 226010, India.
  • 5 Institute für Chemie, Universitat Rostock, Albert Einstein Str. 3a, 18059 Rostock, Germany; Leibniz-Institute für Katalyse an der Universität Rostock e.V., Albert Einstein Str. 29a, 18059 Rostock, Germany.
PMID: 27647368 DOI: 10.1016/j.bmc.2016.08.029
Abstract

Arylated Coumarins were prepared by site-selective Suzuki-Miyaura cross-coupling reaction of the bis(triflate) of 4-methyl-6,7-dihydroxycoumarin. Triarylated Coumarins were prepared by Suzuki-Miyaura cross-coupling reactions of 3-bromo-4-methyl-2-oxo-2H-chromene-6,7-diylbis(trifluoromethanesulfonate). The in vitro anti-HIV activity of the products was investigated. Two lead structures with considerable activities were identified.

Keywords

Anti-HIV activity; Coumarins; Regioselective synthesis; Suzuki–Miyaura cross-coupling reaction.

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