Synthesis 2013; 45(12): 1635-1640
DOI: 10.1055/s-0033-1338468
special topic
© Georg Thieme Verlag Stuttgart · New York

Mild and Selective Organocatalytic Iodination of Activated Aromatic Compounds

Gergely Jakab
Institute of Organic Chemistry, Justus-Liebig University Giessen, Heinrich-Buff-Ring 58, 35392 Giessen, Germany   Fax: +49(641)9934309   Email: prs@uni-giessen.de
,
Abolfazl Hosseini
Institute of Organic Chemistry, Justus-Liebig University Giessen, Heinrich-Buff-Ring 58, 35392 Giessen, Germany   Fax: +49(641)9934309   Email: prs@uni-giessen.de
,
Heike Hausmann
Institute of Organic Chemistry, Justus-Liebig University Giessen, Heinrich-Buff-Ring 58, 35392 Giessen, Germany   Fax: +49(641)9934309   Email: prs@uni-giessen.de
,
Peter R. Schreiner*
Institute of Organic Chemistry, Justus-Liebig University Giessen, Heinrich-Buff-Ring 58, 35392 Giessen, Germany   Fax: +49(641)9934309   Email: prs@uni-giessen.de
› Author Affiliations
Further Information

Publication History

Received: 23 February 2013

Accepted: 17 March 2013

Publication Date:
25 April 2013 (online)


Abstract

We describe an organocatalytic iodination of activated aromatic compounds using 1,3-diiodo-5,5-dimethylhydantoin (DIH) as the iodine source with thiourea catalysts in acetonitrile. The protocol is applicable to a number of aromatic substrates with significantly different steric and electronic properties. The iodination is generally highly regioselective and provides high yields of isolated products. NMR kinetic investigations conducted in THF-d 8 indicate the role of sulfur in the thiourea motif as a nucleophile that is assisted by H-bonding in the key steps of the reaction.

Supporting Information

 
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