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Nickel‐Mediated Radioiodination of Aryl and Heteroaryl Bromides: Rapid Synthesis of Tracers for SPECT Imaging
Author(s) -
Cant Alastair A.,
Champion Sue,
Bhalla Rajiv,
Pimlott Sally L.,
Sutherland Andrew
Publication year - 2013
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201302800
Subject(s) - trifluoroacetic acid , aryl , chemistry , spect imaging , nickel , halogen , single photon emission computed tomography , transformation (genetics) , combinatorial chemistry , radiochemistry , medicinal chemistry , nuclear medicine , organic chemistry , medicine , alkyl , gene , biochemistry
Rapid and efficient radioiodination of aryl and heteroaryl bromides has been achieved using a nickel(0)‐mediated halogen‐exchange reaction. This transformation gives direct access to [ 123 I]‐ and [ 125 I]‐imaging agents for single photon emission computed tomography (SPECT), such as 5‐[ 123 I]‐A85380 (see scheme, Boc= tert ‐butyloxycarbonyl, cod=1,5‐cyclooctadiene, TFA=trifluoroacetic acid).