An optimization study for radioiodination of a new synthesized benzamide derivative as an analogue tracer for malignant melanoma imaging
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Shaban A. Kandil
,
Hany Aglan
Abstract
Iodobenzamides are reported to possess some affinity for melanoma. This study describes the synthesis of a new benzamide analogue, N-(2-diethylamino-ethyl)-4-(4-chloro-nicotinamido)-5-[125I]iodo-2-methoxybenzamide ([125I]H4) designed to target melanoma. The synthesis was simply achieved in four steps. There were two PyCIU/DIPEA amide condensations and a transfer hydrogenation using an ammonium formate hydrogen donor. The radioiodination step was carried out with 125I via an electrophilic substitution reaction. The reaction conditions were optimized. The labeled compound was purified by HPLC. The maximum radiochemical yield was found to be 78% at a radiochemical purity of 98%. All compounds were characterized by MS and NMR techniques. The log P value for [125I]H4 was found as 3.96±0.5.
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Artikel in diesem Heft
- Frontmatter
- Solubility and hydrolysis of Np(V) in dilute to concentrated alkaline NaCl solutions: formation of Na–Np(V)–OH solid phases at 22 °C
- Binuclear trivalent and tetravalent uranium halides and cyanides supported by cyclooctatetraene ligands
- Surface complexation modeling of U(VI) sorption on GMZ bentonite in the presence of fulvic acid
- Evaluation of CNTs/MnO2 composite for adsorption of 60Co(II), 65Zn(II) and Cd(II) ions from aqueous solutions
- An optimization study for radioiodination of a new synthesized benzamide derivative as an analogue tracer for malignant melanoma imaging
- Synthesis, characterization and biological evaluation of a well dispersed suspension of gallium-68-labeled magnetic nanosheets of graphene oxide for in vivo coincidence imaging
- Radio-iodide uptake by modified poly (glycidyl methacrylate) as anion exchange resin
Artikel in diesem Heft
- Frontmatter
- Solubility and hydrolysis of Np(V) in dilute to concentrated alkaline NaCl solutions: formation of Na–Np(V)–OH solid phases at 22 °C
- Binuclear trivalent and tetravalent uranium halides and cyanides supported by cyclooctatetraene ligands
- Surface complexation modeling of U(VI) sorption on GMZ bentonite in the presence of fulvic acid
- Evaluation of CNTs/MnO2 composite for adsorption of 60Co(II), 65Zn(II) and Cd(II) ions from aqueous solutions
- An optimization study for radioiodination of a new synthesized benzamide derivative as an analogue tracer for malignant melanoma imaging
- Synthesis, characterization and biological evaluation of a well dispersed suspension of gallium-68-labeled magnetic nanosheets of graphene oxide for in vivo coincidence imaging
- Radio-iodide uptake by modified poly (glycidyl methacrylate) as anion exchange resin
