A mild method for regioselective labeling of aromatics with radioactive iodine
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...
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| Main Authors: | , , , , , |
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| Format: | Article (Journal) Editorial |
| Language: | English |
| Published: |
May 14, 2013
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| In: |
European journal of organic chemistry
Year: 2013, Issue: 19, Pages: 3970-3973 |
| ISSN: | 1099-0690 |
| DOI: | 10.1002/ejoc.201300419 |
| Online Access: | Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1002/ejoc.201300419 Verlag, lizenzpflichtig, Volltext: https://onlinelibrary.wiley.com/doi/abs/10.1002/ejoc.201300419 
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| Author Notes: | Mads H. Rønnest, Felix Nissen, Palle J. Pedersen, Thomas O. Larsen, Walter Mier, and Mads H. Clausen |
| Summary: | 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. |
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| Item Description: | Gesehen am 19.01.2022 |
| Physical Description: | Online Resource |
| ISSN: | 1099-0690 |
| DOI: | 10.1002/ejoc.201300419 |