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Journal articles on the topic 'IODO DERIVATIVES'

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Published: 5 June 2025
Last updated: 1 August 2025

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1

Edaye, Sonia, Dagobert Tazoo, D. Scott Bohle, and Elias Georges. "3-Halo Chloroquine Derivatives Overcome Plasmodium falciparum Chloroquine Resistance Transporter-Mediated Drug Resistance in P. falciparum." Antimicrobial Agents and Chemotherapy 59, no. 12 (2015): 7891–93. http://dx.doi.org/10.1128/aac.01139-15.

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ABSTRACTPolymorphism in thePlasmodium falciparumchloroquine resistance transporter (PfCRT) was shown to cause chloroquine resistance. In this report, we examined the antimalarial potential of novel 3-halo chloroquine derivatives (3-chloro, 3-bromo, and 3-iodo) against chloroquine-susceptible and -resistantP. falciparum. All three derivatives inhibited the proliferation ofP. falciparum; with 3-iodo chloroquine being most effective. Moreover, 3-iodo chloroquine was highly effective at potentiating and reversing chloroquine toxicity of drug-susceptible and -resistantP. falciparum.
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2

Bacsa, Ildikó, Rebeka Jójárt, János Wölfling та ін. "Synthesis of novel 13α-estrone derivatives by Sonogashira coupling as potential 17β-HSD1 inhibitors". Beilstein Journal of Organic Chemistry 13 (30 червня 2017): 1303–9. http://dx.doi.org/10.3762/bjoc.13.126.

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Novel 13α-estrone derivatives were synthesized by Sonogashira coupling. Transformations of 2- or 4-iodo regioisomers of 13α-estrone and its 3-methyl ether were carried out under different conditions in a microwave reactor. The 2-iodo isomers were reacted with para-substituted phenylacetylenes using Pd(PPh3)4 as catalyst and CuI as a cocatalyst. Coupling reactions of 4-iodo derivatives could be achieved by changing the catalyst to Pd(PPh3)2Cl2. The product phenethynyl derivatives were partially or fully saturated. Compounds bearing a phenolic OH group furnished benzofurans under the conditions
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3

Jovanovic-Santa, Suzana, Vjera Pejanovic, and Julijana Petrovic. "A novel route to 3-hydroxy-16,17-seco-estrone derivatives." Journal of the Serbian Chemical Society 64, no. 5-6 (1999): 391–94. http://dx.doi.org/10.2298/jsc9906391j.

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Starting from 3-benzyloxy-17-hydroxy-16,17-secoestra-1,3,5(10)-triene-16-nitrile (1b), 17-tosylate 2b and also 17-chloro-, 17-bromo- and 17-iodo-derivatives 4b, 5b, and 6b, were obtained. The fluoro-derivative 3b was obtained from2b in the reaction with tetrabutyl ammonium fluoride. The deprotection of the 3-hydroxyl group was achieved by action of hydrogen in presence of Pd/C as a catalyst, yielding six new 3-hydroxy-16,17-seco-estrone derivatives.
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4

Mayooufi, A., M. Romdhani-Younes, and J. Thibonnet. "Efficient One-Pot Synthesis of Triazole-Linked Morpholinone Scaffolds by CuAAC in the Presence of 18-Crown-6." SynOpen 02, no. 04 (2018): 0298–305. http://dx.doi.org/10.1055/s-0037-1610399.

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A range of bis-heterocyclic derivatives based on novel morpholinone­ and triazole heterocycles was prepared from iodo-morpholinone­. The key step in our strategy is a one-pot procedure based upon copper-catalysed alkyne-azide cycloaddition (CuAAC) from iodo-morpholinone.
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5

Luo, Qian, Yongxin Xie, Zhaoyang Chen, et al. "Synthesis of Bis(iodo-benzopyran) Derivatives and Bis(iodo-2H-quinoline) Derivatives by Electrophilic Cyclization." Chinese Journal of Organic Chemistry 34, no. 12 (2014): 2537. http://dx.doi.org/10.6023/cjoc201402019.

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6

Gaikwad, D., R. Murkute, and S. Gaikwad. "Pharmacological Investigation of Fluoro, Iodo and Hydroxy Derivative of Chloro Substituted Homoisoflavonoids." Asian Journal of Organic & Medicinal Chemistry 7, no. 1 (2022): 31–36. http://dx.doi.org/10.14233/ajomc.2022.ajomc-p357.

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In present study, the synthesized substituted homoisoflavonoid derivatives were screened for their in vivo/in vitro antiarthritic activity, in vitro anti-inflammatory and DPPH free radical scavenging activity. The male Wistar rats were used for investigation of in vivo antiarthritic activity against complete freund’s adjuvant (CFA) induced arthritis and assessment was done for change in paw volume, serum marker enzymes (ALP, SGOT and SGPT) and membrane stabilization potential. in vitro anti-inflammatory activity was assessed by the protein denaturation method. In vitro free radical scavenging
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7

Pert, DJ, and DD Ridley. "An Alternative Route to 2-Bromo-Estradiols and 2-Iodo-Estradiols From Estradiol." Australian Journal of Chemistry 40, no. 2 (1987): 303. http://dx.doi.org/10.1071/ch9870303.

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Through careful choice of reaction conditions, alkylation of estradiol with chloromethyl methyl ether may yield either the 3,17β-bis(methoxymethy1) ether or the 3-methoxymethyl ether derivative. Treatment of either of these protected estradiols with s- butyllithium, then with trimethylsilyl chloride affords, regioselectively, the 2-trimethylsilyl derivatives which can conveniently be converted into 2-bromo-or 2-iodo-estradiol.
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8

Chao, Maria, Jean-Michel Chezal, Eric Debiton, et al. "A Convenient Route to New (Radio)Fluorinated and (Radio)Iodinated Cyclic Tyrosine Analogs." Pharmaceuticals 15, no. 2 (2022): 162. http://dx.doi.org/10.3390/ph15020162.

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The use of radiolabeled non-natural amino acids can provide high contrast SPECT/PET metabolic imaging of solid tumors. Among them, radiohalogenated tyrosine analogs (i.e., [123I]IMT, [18F]FET, [18F]FDOPA, [123I]8-iodo-L-TIC(OH), etc.) are of particular interest. While radioiodinated derivatives, such as [123I]IMT, are easily available via electrophilic aromatic substitutions, the production of radiofluorinated aryl tyrosine analogs was a long-standing challenge for radiochemists before the development of innovative radiofluorination processes using arylboronate, arylstannane or iodoniums salts
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9

Carvalho, Mário G. de, Virginia C. da Silva, Tânia M. S. da Silva, Celso A. Camara, and Raimundo Braz-Filho. "New iodine derivatives of flavonol and isoflavone." Anais da Academia Brasileira de Ciências 81, no. 1 (2009): 21–28. http://dx.doi.org/10.1590/s0001-37652009000100004.

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The reaction of the flavonol 3,7,3', 4'-tetra-O-methylquercetin (1) and of the isoflavone 7,4'-di-O-methylgenistein (2) with alkaline iodine in methanol afforded four new iodine derivatives: 8-iodo-5-hydroxy-3,7,3', 4'-tetramethoxy- flavone (1a) and 6-iodo-5-hydroxy-3,7,3', 4'-tetramethoxyflavone (1b) from 1; 2 afforded a mixture of two compounds, identified as a racemic mixture of (±)-trans-5-hydroxy-2,3,7,4'-tetramethoxy-8-iodo-isoflavanone (2a) and (±)-trans-5-hydroxy-2,3,7,4'-tetramethoxy-6,8-diiodo-isoflavanone (2b). The formation of these different products reveals a significant differen
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10

Havelková, Martina, Martin Studenovský, and Dalimil Dvořák. "N1-Substituted Hypoxanthine Derivatives from the Reaction of 6-Halopurines with Michael Acceptors Under the Conditions of Heck Reaction." Collection of Czechoslovak Chemical Communications 65, no. 5 (2000): 797–804. http://dx.doi.org/10.1135/cccc20000797.

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The reaction of 6-iodo-, 9-benzyl-6-chloropurine and 7-benzyl-6-chloropurine with butyl acrylate, acrylonitrile, methyl vinyl ketone or methyl methacrylate under conditions of the Heck reaction in the presence of TlOAc or AgOAc afforded N1-alkylhypoxanthine derivatives. Formation of these unexpected products can be rationalised as a Tl+- or Ag+-assisted substitution of halogen with acetate anion. The 6-acetoxypurine derivative thus formed then eliminates ketene and gives 7-benzyl- or 9-benzylhypoxanthine. Conjugate addition of these compounds onto Michael acceptors furnishes the N1-substituted
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11

Raner, KD, and AD Ward. "Heterocyclic Syntheses Through Electrophilic Ring Closure Reactions of ortho-Allylaniline Systems." Australian Journal of Chemistry 44, no. 12 (1991): 1749. http://dx.doi.org/10.1071/ch9911749.

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Amide derivatives of 2-allylanilines have been prepared by metallation of the amide derivatives of the corresponding 2-bromoanilines and subsequent reaction with an allylic halide. The electrophile -promoted cyclization of these compounds has been investigated. The free allylanilines readily undergo aminomercuration to form unstable mercury derivatives of tetrahydroquinolines but the corresponding amide derivatives do not cyclize. Instead, oxymercuration of the double bond occurs. The allylanilines react with iodine to yield 3-iodo-1,2,3,4-tetrahydroquinolines. The anion of 2,2,2-trifluoro-N-[
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12

Narmadhadevi, V., and Shubashini K Sripathi. "Microwave Synthesis of Iodo Coumarin Derivatives and Antimicrobial Activities of the Products." International Journal of Scientific Engineering and Research 5, no. 2 (2017): 20–23. https://doi.org/10.70729/ijser151228.

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13

Protiva, Jiří, Václav Křeček, Luděk Vlk, et al. "Indirect Iodination of Estrogenes via Triazenes." Collection of Czechoslovak Chemical Communications 58, no. 11 (1993): 2729–36. http://dx.doi.org/10.1135/cccc19932729.

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Triazene derivatives of estrone and estradiol in position 2 and 4 were prepared. Their reaction with sodium iodide in an acid medium afforded the corresponding iodo derivatives. The 1H, 13C NMR and mass spectra of the compound prepared are discussed.
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14

Trainor, RW, GB Deacon, WR Jackson, and N. Giunta. "The Use of Bismuth(III) Acetate in 'Wet' and 'Dry' Prevost Reactions." Australian Journal of Chemistry 45, no. 8 (1992): 1265. http://dx.doi.org/10.1071/ch9921265.

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cis -Diol and trans-diol derivatives can be prepared from alkenes by reaction with iodine and bismuth(III) acetate in 'wet' and 'dry' acetic acid, respectively. Reactions using lesser amounts of bismuth(III) acetate under 'dry' conditions give iodo acetates and under 'wet' conditions a mixture of iodohydrins and iodo ethers. Comparison of these reactions with those promoted by silver, copper, mercury and thallium salts is included.
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15

Al-Matarneh, Cristina Maria, Alina Nicolescu, Ioana Cristina Marinaş, et al. "New Library of Iodo-Quinoline Derivatives Obtained by an Alternative Synthetic Pathway and Their Antimicrobial Activity." Molecules 29, no. 4 (2024): 772. http://dx.doi.org/10.3390/molecules29040772.

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6-Iodo-substituted carboxy-quinolines were obtained using a one-pot, three-component method with trifluoroacetic acid as a catalyst under acidic conditions. Iodo-aniline, pyruvic acid and 22 phenyl-substituted aldehydes (we varied the type and number of radicals) or O-heterocycles, resulting in different electronic effects, were the starting components. This approach offers advantages such as rapid response times, cost-effective catalysts, high product yields and efficient purification procedures. A comprehensive investigation was conducted to examine the impact of aldehyde structure on the sy
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16

Nagy, Enikő, Attila Máriás, Margit Kovács, and Rita Skoda-Földes. "Synthesis of 6- or 8-Carboxamido Derivatives of Imidazo[1,2-a]pyridines via a Heterogeneous Catalytic Aminocarbonylation Reaction." Molecules 29, no. 21 (2024): 5048. http://dx.doi.org/10.3390/molecules29215048.

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Imidazo[1,2-a]pyridines and especially their amide derivatives exhibit a wide range of favourable pharmacological properties. In this work, Pd-catalysed carbonylation was used for the first time for the introduction of the carboxamide moiety into positions 6 or 8. A recyclable Pd catalyst, with palladium immobilised on a supported ionic liquid phase decorated with pyridinium ions, was used efficiently for the conversion of 6- or 8-iodo derivatives to the products. In the case of 6-iodo derivatives, a competing mono- and double carbonylation could be observed in the reactions of aliphatic amine
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17

Cambie, RC, GR Clark, TC Jones, PS Rutledge, GA Strange та PD Woodgate. "vic-Iodo Thiocyanates and Iodo Isothiocyanates. IX. A Synthesis of Penam and Other Polycyclic Β-Lactams". Australian Journal of Chemistry 38, № 5 (1985): 745. http://dx.doi.org/10.1071/ch9850745.

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Penam (4-thia-1-azabicyclo[3.2.0]heptan-7-one) and 2,3-disubstituted penams are prepared conveniently from vic-iodo isothiocyanates beginning with the facile cyclization of the latter with di -t-butyl sodiomalonates. Treatment of the resulting di -t-butyl 2-(thiazolidin-2- ylene ) malonates with trifluoroacetic acid gives t-butyl 2-thiazolin-2- ylacetate derivatives which are reduced to the corresponding thiazolidines with aluminium amalgam. Cleavage of these t-butyl esters with hydrogen chloride affords β-amino acid hydrochlorides, which are cyclized to penam and its derivatives with 1-[3-( d
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18

Kumar, Sonu, Mohammad Mujahid, and Akhilesh K. Verma. "Regioselective 6-endo-dig iodocyclization: an accessible approach for iodo-benzo[a]phenazines." Organic & Biomolecular Chemistry 15, no. 21 (2017): 4686–96. http://dx.doi.org/10.1039/c7ob00671c.

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19

Moriyama, Katsuhiko, Tsukasa Hamada, Kazuma Ishida, and Hideo Togo. "1,3-Iodo-amination of 2-methyl indoles via Csp2–Csp3 dual functionalization with iodine reagent." Chemical Communications 54, no. 34 (2018): 4258–61. http://dx.doi.org/10.1039/c8cc00352a.

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20

Brahim, Mariem, Imen Smari, Hamed Ben Ammar, Bechir Ben Hassine, Jean-François Soulé, and Henri Doucet. "Conditions for palladium-catalyzed direct arylations of 4-bromo and 4-iodo N-substituted pyrazoles without C–Br or C–I bond cleavage." Organic Chemistry Frontiers 2, no. 8 (2015): 917–26. http://dx.doi.org/10.1039/c5qo00093a.

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21

Hou, Yunlei, Liangyu Zhu, Hao Hu та ін. "Iodine promoted iodosulfonylation of alkynes with sulfonyl hydrazides in an aqueous medium: highly stereoselective synthesis of (E)-β-iodo vinylsulfones". New Journal of Chemistry 42, № 11 (2018): 8752–55. http://dx.doi.org/10.1039/c8nj01145a.

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22

Bernhardt, Paul V., Raymond M. Carman, and Tri T. Le. "The Stereo Structures of Some Mycophenolic Acid Derivatives." Australian Journal of Chemistry 60, no. 5 (2007): 354. http://dx.doi.org/10.1071/ch06481.

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23

Tirukovela, Manjula, and Jeyanthi Arasan. "TiI4 Mediated Prins-Type Cyclization of Homoallylic Alcohols and Epoxides: An Efficient Method for the Synthesis of 4-Iodotetrahydropyran Derivatives." DER PHARMA CHEMICA 15, no. 3 (2023): 4. https://doi.org/10.5281/zenodo.10951947.

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24

Pruteanu, Elena, Nicholas D. C. Tappin, Veaceslav Kulciţki, et al. "Forskolin Editing via Radical Iodo- and Hydroalkylation." Synthesis 53, no. 07 (2021): 1247–61. http://dx.doi.org/10.1055/s-0040-1706003.

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AbstractThe modification of highly oxygenated forskolin as well as manoyl and epi-manoyl oxide, two less functionalized model substrates sharing the same polycyclic skeleton, via intermolecular carbon-centered radical addition to the vinyl moiety has been investigated. Highly regio- and reasonably stereoselective iodine atom transfer radical addition (ATRA) reactions were developed. Unprotected forskolin afforded an unexpected cyclic ether derivative. Protection of the 1,3-diol as an acetonide led the formation of the iodine ATRA product. Interestingly, by changing the mode of initiation of th
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25

Hosztafi, Sándor, Márta Kraszni, Gergő Tóth, and János Marton. "Synthesis of 1-Iodo-substituted Codeine Derivatives." Letters in Organic Chemistry 15, no. 12 (2018): 1012–20. http://dx.doi.org/10.2174/1570178615666171222163442.

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26

Rao, Dodla S., Thurpu R. Reddy, Kalvacherla Babachary, and Sudhir Kashyap. "Regioselective vicinal functionalization of unactivated alkenes with sulfonium iodate(i) reagents under metal-free conditions." Organic & Biomolecular Chemistry 14, no. 31 (2016): 7529–43. http://dx.doi.org/10.1039/c6ob01179a.

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A sulfonium iodine(i) electrophilic salt promoted the stereodivergent vicinal bisfunctionalization of a diverse range of alkenes enabling the synthesis of synthetically useful iodo-functionalized derivatives.
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27

Shmal’ko, Akim V., Sergey A. Anufriev, Kyrill Yu Suponitsky, Evgeniia P. Antoshkina, Igor B. Sivaev, and Vladimir I. Bregadze. "Synthesis of B-Substituted Anthracenyl and Pyrenyl Derivatives of ortho-Carborane." Inorganics 13, no. 5 (2025): 138. https://doi.org/10.3390/inorganics13050138.

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Isomeric B-substituted anthracenyl and pyrenyl derivatives of ortho-carborane containing polycyclic aromatic substituents both in the position of the carborane cage most distant from the carbon atoms (position 9) and in the neighboring position (position 3) were synthesized by Pd-catalyzed cross-coupling of the corresponding iodo derivatives of ortho-carborane with polycyclic aryl zinc bromides. The derivative containing two pyrenyl substituents at the positions most distant from the carbon atoms of the ortho-carborane cage, 9,12-di(pyren-1′-yl)-ortho-carborane, was obtained in a similar way s
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28

Ren, Hang, Haoyun An, and Jingchao Tao. "Investigation of 8-Aza-7-Deaza Purine Nucleoside Derivatives." Molecules 24, no. 5 (2019): 983. http://dx.doi.org/10.3390/molecules24050983.

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Glycosylation of 6-amino-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine and its iodo- and bromo- analogues with the protected ribofuranose and 2′-deoxyribofuranose under different conditions resulted in the synthesis of N9- and N8-glycosylated purine nucleosides. Five key intermediate nucleosides, having 6-methoxy, 7-iodo, and 2-bromo groups, were further derivatized to 23 final 8-aza-7-deazapurine nucleoside derivatives. The structures of N9- and N8-glycosylated products were assigned based on UV and NMR spectra. HMBC analysis of 2D NMR spectra and X-ray crystallographic studies of the representative
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29

Barthazy, Peter, Diego Broggini, and Antonio Mezzetti. "Making a 16-electron bromo (or iodo) complex of ruthenium(II) and a C—F bond in one pot." Canadian Journal of Chemistry 79, no. 5-6 (2001): 904–14. http://dx.doi.org/10.1139/v01-049.

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The 16e– bromo or iodo complexes [RuX(dppp)2]+ (dppp = 1,3-bis(diphenylphosphino)propane, X = Br (1c), I (1d)) and [RuX(dppe)2]+ (dppe = 1,2-bis(diphenylphosphino)ethane, X = Br (2c), I (2d)) have been prepared exploiting the reaction of the fluoro complexes [RuF(dppp)2]+ (1a) and [Tl(µ-F)2Ru(dppe)2]+ (3) with activated alkyl bromides or iodides. The X-ray structures of 1c, 1d, 2c, and 2d suggest that the distortion of the Y-shaped trigonal-bipyramidal structure of [MX(P∩P)2]+ is possibly related to the formation of intramolecular hydrogen bonds between the halide ligand and the ortho-hydrogen
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30

Berini, Christophe, Aurélie Lavergne, Valérie Molinier, Stéphane Lebrun, Jean-Marie Aubry, and Eric Deniau. "Asymmetric Iodoetherification of Isosorbide-Derived Glycals: A Regio- and Stereoselective Access to a Variety of O-Substituted Isosorbide Derivatives." Proceedings 41, no. 1 (2019): 62. http://dx.doi.org/10.3390/ecsoc-23-06489.

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Isosorbide is a competitive starting material for various valuable derivatives by functionalization and/or substitution since it is a renewable and carbon neutral material that is produced on an industrial scale from sorbitol. A set of O-alkyl- or O-arylated beta-iodo ethers has been synthesized from isosorbide. The key step was the iodoetherification of isosorbide-derived glycals with a variety of oxygenated nucleophiles in the presence of N-iodosuccinimide. trans-Iodo ethers and acetate were obtained in good yields and the removal of iodide affords isosorbide derivatives. The usefulness of t
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31

Grimaldi, Tamiris B., Guilherme Lutz, Davi F. Back, and Gilson Zeni. "(Biphenyl-2-alkyne) derivatives as common precursors for the synthesis of 9-iodo-10-organochalcogen-phenanthrenes and 9-organochalcogen-phenanthrenes." Organic & Biomolecular Chemistry 14, no. 44 (2016): 10415–26. http://dx.doi.org/10.1039/c6ob01807f.

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We present here our results on the cyclization of (biphenyl-2-ethynyl) selenides to give two different types of phenanthrene derivatives, 9-iodo-10-organochalcogen-phenanthrenes and 9-organochalcogen-phenanthrenes.
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32

Pająk, Małgorzata. "Microwave enhanced synthesis of halogenated derivatives of L-tyrosine labeled with deuterium in aromatic ring." Journal of Radioanalytical and Nuclear Chemistry 326, no. 1 (2020): 857–60. http://dx.doi.org/10.1007/s10967-020-07362-8.

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Abstract Three halogenated derivatives of L-tyrosine, selectively labeled with deuterium in aromatic ring, i.e., 3′-fluoro-[5′-2H]-, 3′-chloro-[5′-2H]-, and 3′-iodo-[2′,5′-2H2]-L-tyrosine, were synthesized using microwave assisted acid-catalyzed isotope exchange between 3′-fluoro-, 3′-chloro- and 3′-iodo-L-tyrosine and heavy water. The degree of deuterium incorporation was confirmed by 1H NMR spectroscopy. The spectroscopic data indicate that isotope exchange depends on the method of heating and the power of microwaves. The deuterium enrichment of 3′-fluoro-[5′-2H]- and 3′-chloro-[5′-2H]-L-tyr
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33

Hervé, Gwénaëlle, and Christophe Len. "First ligand-free, microwave-assisted, Heck cross-coupling reaction in pure water on a nucleoside – application to the synthesis of antiviral BVDU." RSC Adv. 4, no. 87 (2014): 46926–29. http://dx.doi.org/10.1039/c4ra09798j.

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For the first time, a palladium catalyzed Heck cross-coupling reaction between 5-iodo-2′-deoxyuridine and various acrylate derivatives was performed using ligand-free conditions and microwave assistance in pure water.
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34

Bobokhidze, Lia. "NOVEL SYNTHETIC INVESTIGATION IN THE FIELD OF INDOLO[2,3-B]QUINOXALINE RING CONTAINING TETRACYCLIC AND PENTACYCLIC HETEROCYCLES." New Materials, Compounds and Applications 8, no. 1 (2024): 13–23. http://dx.doi.org/10.62476/nmca8113.

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A series of seven new indolo[2,3-b]quinoxaline ring containing compounds were efficiently synthesized in three different pathways. In the first case, the relevant pentacyclic systems (3,4) were received by the condensation reaction between 7-acetyl-1,5,6,7-tetrahydropyrrolo[3,2-f]indole-2,3-dione and o-phenylenediamine in glacial acetic acid. In the second case, tetracyclic indolo[2,3-b]qui-no¬xa¬li¬ne derivatives (7, 8a-d) were synthesised by a one-pot approach using Pd-catalyzed Sonogashira-hagihara C-C cross-coupling reaction between various terminal acetylenes and 9-iodo-6H-indo¬lo¬[2,3-b]
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35

Kawamura, Yasuhiko, Masashi Maruyama, Kazuyo Yamashita, and Masao Tsukayama. "Environmentally Benign Synthesis of Isoflavone Derivatives Using Polymer-Supported Hypervalent Iodine(III) Reagent." International Journal of Modern Physics B 17, no. 08n09 (2003): 1482–86. http://dx.doi.org/10.1142/s0217979203019198.

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Isoflavones are synthesized in one-pot manner by action of a hypervalent iodine (III) reagent, ⌊hydroxy(tosyloxy)iodo⌋benzene (HTIB, Koser's reagent) on 2'-benzoyloxychalcones in MeOH. A combined usage of iodobenzene diacetate (IBD)—p-toluenesulfonic acid (TsOH) is also effective for the same purpose. As an extension of those monomeric reagents, polymer-supported IBD (PSIBD, poly ⌊4-(diacetoxy)iodo⌋styrene) with TsOH works also well with merit of easy separation of isoflavones from the reaction mixture, no liberation of PhI, and reuse of the reagent.
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36

Hunter, Luke, and Craig A. Hutton. "Preparation of Selectively Protected L-Dopa Derivatives: Oxidation of Tyrosine-3-boronates." Australian Journal of Chemistry 56, no. 11 (2003): 1095. http://dx.doi.org/10.1071/ch03181.

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Conversion of 3-iodo-L-tyrosine to protected tyrosine-3-boronate esters, followed by oxidation with hydrogen peroxide, provides a mild and efficient method for the preparation of selectively protected L-dopa derivatives.
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37

Magwaza, Nontokozo M., Garland K. More, Samantha Gildenhuys та Malose J. Mphahlele. "In Vitro α-Glucosidase and α-Amylase Inhibition, Cytotoxicity and Free Radical Scavenging Profiling of the 6-Halogeno and Mixed 6,8-Dihalogenated 2-Aryl-4-methyl-1,2-dihydroquinazoline 3-Oxides". Antioxidants 12, № 11 (2023): 1971. http://dx.doi.org/10.3390/antiox12111971.

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Series of the 6-bromo/iodo substituted 2-aryl-4-methyl-1,2-dihydroquinazoline-3-oxides and their mixed 6,8-dihalogenated (Br/I and I/Br) derivatives were evaluated for inhibitory properties against α-glucosidase and/or α-amylase activities and for cytotoxicity against breast (MCF-7) and lung (A549) cancer cell lines. The 6-bromo-2-phenyl substituted 3a and its corresponding 6-bromo-8-iodo-2-phenyl-substituted derivative 3i exhibited dual activity against α-glucosidase (IC50 = 1.08 ± 0.02 μM and 1.01 ± 0.05 μM, respectively) and α-amylase (IC50 = 5.33 ± 0.01 μM and 1.18 ± 0.06 μM, respectively)
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38

Vetriselvan, Moorthy, Manickam Pramesh, Selvaraj Jayanthi, and Ponnusamy Shanmugam. "One Pot Synthesis of 6-Phenyl-pyrazolyl-quinzolinone Derivatives using Palladium Catalyst via Suzuki-Miyaura Cross-Coupling Reaction." Asian Journal of Chemistry 34, no. 4 (2022): 953–58. http://dx.doi.org/10.14233/ajchem.2022.23674.

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In present work, a palladium-mediated Suzuki-Miyaura cross-coupling reaction, which enables the efficient synthesis of 6-phenyl-pyrazolyl-quinzolinone derivatives from 6-iodo-pyrazolyl-quinzolinone, aryl boronic acid with potassium carbonate (K2CO3) is described.
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39

Li, Qingjiang, Jiatong Guo, and Zhongwu Guo. "Direct access to various C3-substituted sialyl glycal derivatives from 3-iodo-sialyl glycals." Organic & Biomolecular Chemistry 19, no. 46 (2021): 10169–73. http://dx.doi.org/10.1039/d1ob01977e.

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Sialyl glycal C3-aryl, alkyl, alkenyl, and alkynyl derivatives useful for sialylidase inhibitor discovery were efficiently synthesized by a new method based on the cross-coupling of 3-iodo-sialyl glycal with boronic acids, alkenes, and alkynes.
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40

Salma, A., Sherbeni El, Tarek, F., and Moselhy El. "Computational Evaluation of the Druggability and Biological Activity of Iodo-1,4-dihydropyridine Derivatives." Chemistry Research Journal 2, no. 5 (2017): 131–41. https://doi.org/10.5281/zenodo.13950955.

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Several successful antihypertensive medicines already in clinical use are derivatives of 1,4-dihydropyridine (1,4-DHP). They are considered the most potent calcium channel blockers of which, nitro-, chloro- and fluro-1,4-DHP derivatives have been extensively investigated for biological activity [1-5]. Nevertheless, iodo-1,4-DHP derivatives have not received enough attention. Our aims were to evaluate the druglikeness and bioactivity of a new series of 2- & 3-iodophenyl-2,6-dimethyl-1,4-dihydropyridine derivatives using Molispiration software, as well as to dock these derivatives into the a
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41

Talybov, G. М. "Synthesis and intramolecular cyclization of propargyl ethers derived from 1-bromo(iodo)-3-organyloxy-2-propanol." Voprosy Khimii i Khimicheskoi Tekhnologii, no. 1 (February 2025): 80–85. https://doi.org/10.32434/0321-4095-2025-158-1-80-85.

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The interaction of bromine (iodine)-releasing reagents, such as N-bromosuccinimide (NBS) or a mixture of iodine and clinoptilolite ((NaK)4CaAl6Si30O72), with an equimolar mixture of 3-organyloxy-1-propene and propynol results in the formation of propargyl ethers of 1-bromo(iodo)-3-organyloxy-2-propanol. The outcome of the catalytic hydration reaction of these ethers depends on the halogen atom present. Bromo derivatives are converted into the expected keto-bromo ethers, whereas iodo derivatives undergo simultaneous hydrolysis of the C–I bond and intermolecular ketalization, forming hydroxy der
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42

Nwachukwu, Chideraa I., Nathan P. Bowling та Eric Bosch. "C—I...N and C—I...π halogen bonding in the structures of 1-benzyliodoimidazole derivatives". Acta Crystallographica Section C Structural Chemistry 73, № 1 (2017): 2–8. http://dx.doi.org/10.1107/s2053229616018702.

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Halogen bonding is a well-established and intensively studied intermolecular interaction that has also been used in the preparation of functional materials. While polyfluoroiodo- and polyfluorobromobenzenes have been widely used as aromatic halogen-bond donors, there have been very few studies of iodoimidazoles with regard to halogen bonding. We describe here the X-ray structures of three iodoimidazole derivatives, namely 1-benzyl-2-iodo-1H-imidazole, C10H9IN2, (1), 1-benzyl-4-iodo-1H-imidazole, C10H9IN2, (2), and 1-benzyl-2-iodo-1H-benzimidazole, C14H11IN2, (3), and the halogen bonds that dom
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43

Sahoo, Akhila, Sanatan Nayak, B. Prabagar, Nayan Ghosh, and Rajendra Mallick. "Ag(I)-Catalyzed Cycloisomerization and Cyclization of Ketene Aminals: Construction of Azepine and 1,2-Dihydropyridine Derivatives." Synthesis 49, no. 18 (2017): 4261–71. http://dx.doi.org/10.1055/s-0036-1588841.

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Silver-catalyzed cyclization and cycloisomerization of ketene N,N-acetals at room temperature has been developed to access a variety of highly substituted cyclobutene-fused azepine and 1,2-dihydropyridine derivatives. This cost-effective method is reliably implemented for the gram-scale synthesis of azepine and dihydropyridine derivatives. The iodo group in the periphery of the dihydropyridine motif can be functionalized with both Suzuki and Sonogashira reactions.
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44

Rádl, Stanislav, Ondřej Klecán, Robert Klvaňa, and Jaroslav Havlíček. "A New Synthesis of Rizatriptan Based on Radical Cyclization." Collection of Czechoslovak Chemical Communications 73, no. 1 (2008): 116–26. http://dx.doi.org/10.1135/cccc20080116.

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A new methodology useful for preparation of indole derivatives bearing a 2-(dialkylamino)-ethyl substituent at the 3-position has been developed. Application of this methodology to the synthesis of N,N-dimethyl-2-{5-[(1H-1,2,4-triazol-1-yl)methyl]-1H-indol-3-yl}ethan-1-amine (rizatriptan; 3) is described. The key reaction step is based on the radical cyclization of N-[4-(dimethylamino)but-2-yn-1-yl]-N-{2-iodo-4-[(1H-1,2,4-triazol-1-yl)methyl]phenyl}-acetamide (21), easily available by the Mannich reaction, and subsequent isomerization of the primarily formed methylidene derivative 22.
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45

Penov-Gasi, Katarina, Srdjan Stojanovic, Marija Sakac, et al. "Synthesis, crystal structure and antiaromatase activity of 17-halo-16,17-seco-5-androstene derivatives." Journal of the Serbian Chemical Society 68, no. 10 (2003): 707–14. http://dx.doi.org/10.2298/jsc0310707p.

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Starting from 3?-acetoxy-15-cyano-17-oxo-16,17-seco-5-androstene (2) and 3?-acetoxy- 15-cyano-17-hydroxy-17-methyl-16,17-seco-5-androstene (11), new 17-halo-derivatives (5?10 and 13) were obtained. The fluoro derivative 5 was obtained from 17-tosylate 4 in reaction with tetrabutylammonium fluoride. The structure of the 17-iodo-devitive 10 was unambiguously proved by the appropriate X-ray structural analysis. Compounds5?10, as well as 12 and 13 were tested for possible anti-aromatase activity, whereby only compound 9 with bromine as the C-17 substituent, induced 19.4 % inhibition of aromatase a
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46

DeShong, Philip, Christopher J. Handy, and Molly E. Mowery. "Hypervalent siloxane derivatives. An alternative to Stille and Suzuki couplings." Pure and Applied Chemistry 72, no. 9 (2000): 1655–58. http://dx.doi.org/10.1351/pac200072091655.

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Siloxane methodology is extended to couplings with iodo- and bromoanilines, hindered arylbromides, and substituted siloxanes as substrates. Additionally, initial studies with 5-bromoindole and other heteroaromatics suggest that the siloxane-mediated cross coupling methodology will also be applicable in these systems.
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47

V, Vijay, Manjusha V. Karkhelikar, B. Sridhar, Nedaossadat Mirzadeh, Suresh Bhargava, and Pravin R. Likhar. "Electronically modified amine substituted alkynols for regio-selective synthesis of dihydrofuran derivatives." Organic & Biomolecular Chemistry 14, no. 1 (2016): 288–95. http://dx.doi.org/10.1039/c5ob02033f.

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48

Shmal’ko, Akim V., Sergey A. Anufriev, Kyrill Yu Suponitsky, and Igor B. Sivaev. "How to Protect ortho-Carborane from Decapitation—Practical Synthesis of 3,6-Dihalogen Derivatives 3,6-X2-1,2-C2B10H10 (X = Cl, Br, I)." Inorganics 10, no. 11 (2022): 207. http://dx.doi.org/10.3390/inorganics10110207.

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The 3-halogen and 3,6-dihalogen derivatives of ortho-carborane 3-X-1,2-C2B10H11 and 3,6-X2-1,2-C2B10H10 (X = Cl, Br, I) were prepared by Cu-assisted halodeboronation of the corresponding pinacolborate derivatives 3-Bpin-1,2-C2B10H11 and 3,6-(Bpin)2-1,2-C2B10H10. It was shown that decapitation of 3-Cl-1,2-C2B10H11, similarly to the corresponding bromo and iodo derivatives, proceeds regioselectively with the retention of the B-Cl bond. Crystal structures of 3,6-Cl2-1,2-C2B10H10 and Cs [3-Cl-7,8-C2B9H11] were determined by single crystal X-ray diffraction.
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49

Li, Yawen, Ming-Kuan Chyan, Donald K. Hamlin, Holly Nguyen, Eva Corey, and D. Scott Wilbur. "Oxidation of p-[125I]Iodobenzoic Acid and p-[211At]Astatobenzoic Acid Derivatives and Evaluation In Vivo." International Journal of Molecular Sciences 23, no. 18 (2022): 10655. http://dx.doi.org/10.3390/ijms231810655.

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The alpha particle-emitting radionuclide astatine-211 (211At) is of interest for targeted radiotherapy; however, low in vivo stability of many 211At-labeled cancer-targeting molecules has limited its potential. As an alternative labeling method, we evaluated whether a specific type of astatinated aryl compound that has the At atom in a higher oxidation state might be stable to in vivo deastatination. In the research effort, para-iodobenzoic acid methyl ester and dPEG4-amino acid methyl ester derivatives were prepared as HPLC standards. The corresponding para-stannylbenzoic acid derivatives wer
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50

Ghosez, Léon, Cécile Franc, Frédéric Denonne, Claire Cuisinier, and Roland Touillaux. "Studies of palladium-catalyzed coupling reactions for preparation of hindered 3-arylpyrroles relevant to (-)-rhazinilam and its analogues." Canadian Journal of Chemistry 79, no. 11 (2001): 1827–39. http://dx.doi.org/10.1139/v01-156.

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Suzuki cross-coupling reactions of 3-pyrroleboronic acid derivatives with haloaromatics and the reverse process i.e., the coupling of 3-iodo(bromo)pyrroles with arylboronic acids have been investigated as a potential key step in the synthesis of (–)-rhazinilam and analogues. It was found that 3-iodo-2-formyl-1-tosylpyrroles efficiently coupled with a variety of arylboronic acids in the presence of PdCl2(dppf) as catalyst. This catalytic system is compatible with a broad spectrum of arylboronic acids — electron-rich, electron-poor, hindered, heterocyclic — which easily coupled with the pyrrole
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