☆ 4.4 Article

ZnO-mediated regioselective C-arylsulfonylation of indoles: a facile solvent-free synthesis of 2- and 3-sulfonylindoles and preliminary evaluation of their activity against drug-resistant mutant HIV-1 reverse transcriptases (RTs)

TETRAHEDRON LETTERS (2013)

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Journal

TETRAHEDRON LETTERS
Volume 54, Issue 46, Pages 6237-6241

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2013.09.017

Keywords

Regioselectivity; C-Arylfonylation; Indoles; Non-nucleoside inhibitor; HIV-1 RT

Categories

Chemistry, Organic

Funding

  1. Ministero dell'Universita, dell'Istruzione e della Ricerca MIUR
  2. RAS [LR 7/2007 CRP-24915]

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A ZnO-mediated one-pot solvent-free protocol for the regioselective C-arylsulfonylation of indoles is described and some novel derivatives were tested on wild type and non-nucleoside inhibitor resistant K103N and Y181C HIV-1 reverse transcriptases (RTs). (C) 2013 Elsevier Ltd. All rights reserved.

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