Journal article
A Mild Method for Regioselective Labeling of Aromatics with Radioactive Iodine : Regioselective Labeling of Aromatics with Radioactive Iodine
Department of Systems Biology, Technical University of Denmark1
Department of Chemistry, Technical University of Denmark2
Organic Chemistry, Department of Chemistry, Technical University of Denmark3
Center for Nanomedicine and Theranostics, Centers, Technical University of Denmark4
University Hospital Heidelberg5
Center for Microbial Biotechnology, Department of Systems Biology, Technical University of Denmark6
A novel technique to label ortho‐, meta‐, and para‐trimethylsilyl‐substituted aryl substituents with radioactive iodide is described. The method takes advantage of the ipso‐directing and activating properties of trimethylsilyl substituents on the arenes. The method was demonstrated on a griseofulvin analogue with promising anticancer properties and on lidocaine, a widely used local anesthetic drug.
Treatment of a trimethylsilyl precursor with Tl(OCOCF3)3 followed by Na125I consistently afforded radioactive purities over 95 % in all cases.
| Language: | English |
|---|---|
| Publisher: | WILEY‐VCH Verlag |
| Year: | 2013 |
| Pages: | 3970-3973 |
| ISSN: | 10990690 and 1434193x |
| Types: | Journal article |
| DOI: | 10.1002/ejoc.201300419 |
| ORCIDs: | Larsen, Thomas Ostenfeld and Clausen, Mads Hartvig |
