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Radioiodinated aliphatic amines as potential pulmonary imaging agents: II. Synthesis of ω‐(4‐[ 131 I]‐iodophenyl)pentylamine and its β‐ and γ‐Methyl substituted analogues
Author(s) -
Lee Y. W.,
Gopalakrish G.,
Man S. F. P.,
Noujaim A. A.
Publication year - 1988
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.2580250605
Subject(s) - chemistry , yield (engineering) , alkyl , chemical synthesis , halogenation , organic chemistry , radiochemistry , medicinal chemistry , in vitro , biochemistry , materials science , metallurgy
The aliphatic amines, ω‐phenylpentylamine and its β‐methyl substituted analogue were synthesized from ω‐phenylpentanoic acid in 34.7% and 28.5% overall chemical yield respectively. γ‐Methyl‐ω‐phenylpentylamine was prepared from ω‐phenylbutyric acid in 39.5% overall chemical yield. Radioiodination of the amines with thallium trifluoroacetate and no‐carrier‐added [ 131 I]‐NaI afforded the corresponding [ 131 I]‐labelled amines in 30%, 28% and 36% radiochemical yield respectively and greater than 98% radiochemical purity (calculated specific activity 20 – 40 TBqmmol −1 ). The position of iodination was established by proton magnetic resonance to be para to the alkyl chain.