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

被引：0
作者：
Garnes, KT [1 ]
Landvatter, SW [1 ]
Gallagher, TF [1 ]
机构：
[1] SMITHKLINE BEECHAM PHARMACEUT,DEPT MED CHEM,KING OF PRUSSIA,PA 19406
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1996年 / 38卷 / 07期
关键词：
pyridinyl imidazole; CSAID(TM); iodine-125; photoaffinity labelling;
D O I：
10.1002/(SICI)1099-1344(199607)38:7<637::AID-JLCR871>3.0.CO;2-T
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
The pyridinyl imidazole cytokine-suppressing anti-inflammatory drug (CSAID(TM)), SB 206718 (1) was required in I-125-labeled form for photoaffinity ligand studies. The target compound (SE 206718-[I-125], [I-125]1) was obtained via conversion of the highly functionalized 1 to a tributylstannyl derivative. Radioiododestannylation using (NaI)-I-125 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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收藏
页码：637 / 643
页数：7
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