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Synthesis of an [ 125 I]‐labelled derivative of MK‐571, a tool for LTD 4 receptor studies
Author(s) -
Li ChunSing,
Leblanc Yves,
Zamboni Robert,
Young Robert N.
Publication year - 1994
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580340607
Subject(s) - chemistry , derivative (finance) , yield (engineering) , thio , alcohol , chemical synthesis , medicinal chemistry , stereochemistry , organic chemistry , in vitro , biochemistry , materials science , financial economics , economics , metallurgy
An [ 125 I]‐labelled derivative of MK‐571 2 was synthesized from the arylstanne derivative 11 in 50% radiochemical yield. Compound 2 is a useful tool for LTD 4 receptor studies. The arylstanne intermediate 11 was obtained from the coupling reaction of (±)‐3‐[[[3‐[2‐(7‐chloro‐2‐quinolinyl)‐(E)‐ethenyl]phenyl][[3‐[(3‐aminopropyl)amino]‐3‐oxopropyl]thio]methyl]thio]propionic acid 10 with N‐hydroxysuccinimidyl 4‐trimethylstannylphenylacetate 3 . The synthesis of 3 could be easily achieved from 4‐bromophenethyl alcohol.