Radioiodinated aliphatic amines as potential pulmonary imaging agents: III. Synthesis of 6-[131i]-iodohexylamine and its β-alkyl substituted analogues
✍ Scribed by G. Gopalakrishna; Y. W. Lee; S. Selvaraj; D. N. Abrams; S. F. P. Man; A. A. Noujaim
- Publisher
- John Wiley and Sons
- Year
- 1988
- Tongue
- French
- Weight
- 543 KB
- Volume
- 25
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
The aliphatic amines. 2-methyl-and 2-isopropyl-substituted 6-hydroxy-1-hexylamines were synthesized from ethyl-6-hydroxyhexanoate in 22% and 11% overall chemical yield respectively. 6-hydroxy-1 -hexylamine was available commercially. 6-hydroxy -l -hexylamine and its 2-methyl-and 2-isopropyl-substituents were successfully radioiodinated with trimethylsilyl polyphosphate and [1311]-NaI/Nal to afford the corresponding 6-[1311]-labelled amines in 672. 6 1 8 and 55% radiochemical yield respectively and greater than 982 radiochemical purity (specific activity 340 CJ3q mmol-l). licy words: radioiodination. jodohexanes. PPSE. MAO. pulmonary. l3lI.
Introduction
Lung injury and discavs due to many widely different causative agents can result in a compromise of gaseous exchange function. Conventional nuclear and non-nuclear diagnostic procedure suffer the drawbacks of a lack of sensitivity and. may be. specificity. For this reason, there is a need for diagnostic tests that are capable of detecting long injury at an early stage. While the pathogenesis of lung injury remains unclear, damage to the endothelial cells, among other cell types, have been implicated in many Besides gaseous exchange. the lung is also involved in certain non-respiratory functions.
Compoucds as different as peptides, amines. nucleosides and lipids are hydrolyzed, oxidized and/or taken up by :he lungs, a iunction which is directly related to the endothelial cell n ~m b e r ~. ~* ~* ~.
The endothelial cells are the single most common cell type in the lung, representing up to W of the total lung cells. If endothelial cell damage is indeed an important initiating event in the pathogenesis of some lung injury, early injury may be reflected in a loss of endothelial cell functions and consequently, a n impairment in their barrier and metabolic function^'.^^^^^^^^^^^^. Gillis and Catravas' have established that the rate of
📜 SIMILAR VOLUMES
The aliphatic amines. o-phenylpmylamine and its 8-methyl substituted analogue were synthesized from o-phenylpentanoic acid in 34.7% and 28.5% overall chemical yield rcspectivcly. y -Methyl -a-phenylpentylamine was prepared from o-phenylbutyric acid in 39.5% overall chemical yield. Radioiodination of