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Synthesis of 4-[2-(4-Azidophenyl)-5-(3-iodo-125I-phenyl)-1H-imidazol-4-yl]pyridine (SB 206718-[125I]), a pyridinyl imidazole cytokine inhibitor

โœ Scribed by Keith T. Garnes; Scott W. Landvatter; Timothy F. Gallagher


Publisher
John Wiley and Sons
Year
1996
Tongue
French
Weight
345 KB
Volume
38
Category
Article
ISSN
0022-2135

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โœฆ Synopsis


The pyridinyl imidazole cytokine-suppressing anti-inflammatory drug (CSAID"), SB 206718 (1) was required in 1251-labeled form for photoaffinity ligand studies. The target compound (SB 206718-[1251], [1*5I]l) was obtained via conversion of the highly functionalized 1 to a tributylstannyl derivative. Radioiododestannylation using Na125I in the presence of chloramine-T gave good radiochemical yields of the title compound (42-69%, four radiosyntheses) at high radiochemical purity (>98%) after HPLC purification at specific activities of 1670-1736 Ci/mmol.


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