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Nonisotopic Labeling
Published in Lelio G. Colombetti, Principles of Radiopharmacology, 2019
The iodine chloride procedure was one of the early methods developed for iodination of proteins (Figure 1).15 It consists of the equilibration of 125I (or other radioiodine isotope) as the iodide with ICI in HCl solution. 125I CI is formed in amounts depending on the molar ratios of the ICI and Na 125I present. Since unlabeled ICI is always present, the specific activity of the labeled protein is lower than with some other methods. The 125I CI is quickly jetted into a solution of protein buffered to around pH 8.0. The iodination takes place rapidly and the unreacted ICI is hydrolyzed to a nonreactive state. Some proteins, such as insulin, may be iodinated by this method in an acid medium.15 High specific activity iodinations have been reported by direct preparation of labeled ICI.17 The iodine monochloride is a mild procedure and gives labeled proteins, which usually retain the original biological properties.
Chemistry and Isotopes of Iodine
Published in Erwin Regoeczi, Iodine-Labeled Plasma Proteins, 2019
Of practical importance in this group of compounds is iodine monochloride (IC1, mol wt 162.35) because it is the backbone of a widely used iodination procedure. It is a low-melting red solid that, in the molten state, conducts electricity. IC1 in solution (1 M HC1) has a characteristic, pale yellow color. IC1 is stable at low pH but it hydrolyzes rapidly as the pH is increased. Preparation and further properties of IC1 are discussed in Chapter 3.
Principles of Radioiodination and Iodine-Labeled Tracers in Biomedical Investigation †
Published in Garimella V. S. Rayudu, Lelio G. Colombetti, Radiotracers for Medical Applications, 2019
Mrinal K. Dewanjee, Shyam A. Rao
Bromsulphalein (BSP) is similar to rose bengal and can be labeled with 131I.143,131I-BSP can be labeled by two methods. The first method was described by Meyers144 and uses iodine monochloride. In the second method, 131I is introduced into the compound by “exchange” of some of the bromine in BSP (Figure 25). The iodine monochloride method gave better yields and a higher specific activity, 137.8 μCi/mg of dye. More recently, Suwanik et al.145,146 described both a simplified method of preparing 131I-BSP by the IC1 method and its usefulness as a liver-scanning agent.
Discovery of polymethoxyflavones as potential cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX) and phosphodiesterase 4B (PDE4B) inhibitors
Published in Journal of Receptors and Signal Transduction, 2022
Muhd Hanis Md Idris, Siti Norhidayah Mohd Amin, Siti Norhidayu Mohd Amin, Agustono Wibowo, Zainul Amiruddin Zakaria, Zurina Shaameri, Ahmad Sazali Hamzah, Manikandan Selvaraj, Lay Kek Teh, Mohd Zaki Salleh
All the compounds were synthesized according to the steps outlined in Figure 1. The chalcone derivatives (C1, C3, C4, and C5) were prepared via Claisen–Schmidt condensation reaction of readily accessible acetophenones and benzaldehydes in the presence of 20% sodium hydroxide in ethanol at room temperature for 24 h. While synthesis of chalcone derivatives C2 begun through iodonization of 4,6-dimethoxy-2-hydroxy-acetophenone with iodine monochloride in dry acetone at room temperature for 5 h. Targeting flavones (F1–F5) were synthesized by refluxing corresponding chalcones in DMSO in the presence of iodine as catalyst. All the synthesized flavones were confirmed on the basis of their spectroscopic evidence. In the 1H NMR spectra of F1–F5, olefinic proton attached to the C-3 appeared as a singlet in the range of δH 5.69–6.90, while singlet signals from methoxy protons appeared at δH 3.87–4.03. Besides that, aromatic protons attached to the ring A and C appeared as a singlet, doublet and multiplate in the range of δH 5.28–8.13.
Aryl derivatives of 3H-1,2-benzoxathiepine 2,2-dioxide as carbonic anhydrase inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Aleksandrs Pustenko, Alessio Nocentini, Anastasija Balašova, Ahmed Alafeefy, Mikhail Krasavin, Raivis Žalubovskis, Claudiu T. Supuran
The synthesis of desired compounds is partly based on the strategy previously developed by our groups10. The synthesis of 7-aryl 3H-1,2-benzoxathiepine 2,2-dioxides starts with the iodination of salicylaldehyde (1) by iodine monochloride and corresponding iodo derivative 2 was isolated in good yield (Scheme 1)11. Under Wittig reaction conditions aldehyde 2 was converted to olefin 3, which was treated by sulphonyl chloride 4 thus providing bis-olefin 5 in 83% yield. To obtain the key intermediate 7, the ring closure in compound 5 was performed in olefin metathesis conditions, using Ru-catalyst 6. The key intermediate 7 was reacted with a series of aryl boronic acids under Suzuki reaction conditions and the desired 7-aryl 3H-1,2-benzoxathiepine 2,2-dioxides 8–12 were isolated in acceptable yields (44–66%) (Scheme 1).