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.

引用

页码：637 / 643

页数：7