87956-05-6

Upstream product

• 27389-55-5 N,N,N-trimethyl-3-nitroanilinium iodide 
• 99-65-0 meta-dinitrobenzene 
• 100-25-4 para-dinitrobenzene 
• 585-79-5 m-nitrobromobenzene 
• 98-46-4 3-trifluoromethylnitrobenzene 
• 16825-78-8 1-iodoxy-3-nitrobenzene 
• 110441-18-4 (4-methoxyphenyl)(3'-nitrophenyl)iodonium tosylate 
• 99-09-2 3-nitro-aniline 
• 68716-48-3 4,4,5,5-tetramethyl-2-(3-nitrophenyl)-1,3,2-dioxaborolane 
• 645-00-1 m-iodonitrobenzene 
• 1330786-73-6 (5-methyl-2-thienyl)(3-nitrophenyl)iodonium tosylate 
• 1330786-71-4 (3-nitrophenyl)(2-thienyl)iodonium tosylate 

Relevant academic research and scientific papers

Radiofluoridations of m-substituted nitrobenzenes

The fluoridation of a range of m-substituted nitrobenzenes with no-carrier-added [18F]fluoride was investigated. Electron-deficient m-substituted nitrobenzenes react with no-carrier-added [18F]fluoride to give 18F-labelled m-disubstituted benzenes in low

A general protocol for Cu-mediated fluoro-deamination: Sandmeyer fluorination of diverse aromatic substrates

A Cu(I)-mediated fluoro-deamination method for nucleophilic radiofluorination was devised. The method affords fluorinated aromatic products directly from anilines under both no-carrier added and stoichiometric conditions. Isolated radiochemical yields ran

Chemoselective Radiosyntheses of Electron-Rich [18F]Fluoroarenes from Aryl(2,4,6-trimethoxyphenyl)iodonium Tosylates

Hypervalent diaryliodonium salts have been used to produce various [18F]fluoroarenes. The iodonium salt approach as a labeling precursor has been established to equally afford complex 18F-fluorinated molecules. Because of the inheren

Catalyst-Free Aromatic Radiofluorination via Oxidized Iodoarene Precursors

Oxidized iodoarenes (OIAs), prepared via mCPBA-mediated oxidation, have been demonstrated as versatile precursors for the synthesis of [18F]fluoroarenes in the absence of catalysts. OIAs have been identified as intermediates in single-pot syntheses of iodonium salts and ylides but have never been recognized as radiofluorination precursors. Here, the isolated OIAs were used without any catalysts to produce functionalized [18F]fluoroarenes, regardless of the electronic nature of the arenes. This method was also applied to the production of radiolabeling synthons for use as aromatic 18F-labeled building blocks.

FLUORINATION METHOD

The present invention relates to a process for producing an organic compound comprising an 18F atom. The compounds comprising an 18F can be useful as PET ligands for use in diagnostics and/or scanning. The process of the invention comprises treating an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp2 hybridised carbon atom, with (i) 18F – and (ii) a copper compound. The invention also provides the use of an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp2 hybridised carbon atom, in a process for producing an organic compound comprising an 18F atom, which process comprises treating the organoboron compound with (i) 18F – and (ii) a copper compound. The invention also provides a compound of formula (XXXVII): wherein: each PGA is independently H or an alcohol protecting group; PGB is H or a carboxylic acid protecting group; each PGC is independently an amine protecting group; Z is a group selected from a boronic ester group, a boronic acid group, a borate group, and a trifluoroborate group; and a is an integer from 0 to 4.

Radiofluorination of diaryliodonium tosylates under aqueous-organic and cryptand-free conditions

Positron emission tomography (PET) has growing importance as a molecular imaging technique in clinical research and drug development. Methods for producing PET radiotracers utilizing cyclotron-produced [18F]fluoride ion (t1/2 = 109.7

Rapid and efficient radiosyntheses of meta-substituted [ 18F]fluoroarenes from [18F]fluoride ion and diaryliodonium tosylates within a microreactor

Effective methods for the introduction of the short-lived positron-emitter fluorine-18 (t1/2 = 109.7 min) at high specific radioactivity into fluoroarenes are valuable for the development of radiotracers for molecular imaging with positron emis

Metabolic stability of 6,7-dialkoxy-4-(2-, 3- and 4-[18F] fluoroanilino)quinazolines, potential EGFR imaging probes

Epidermal growth factor receptors (EGFR), upregulated in many tumor types, have been a target for therapeutic development and molecular imaging. The objective of this study was to evaluate the distribution and metabolic characteristics of fluorine-18 labe

NUCLEOPHILIC FLUORINATION OF AROMATIC COMPOUNDS

Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO2) is regiospecifically substituted by nucleophilic fluoride to provide the corresponding fluoroaryl derivatives. No-carrier-added [F-18] fluoride ion derived from anhydrous [F- 18]KF/Kryptofix, [F-18]CsF or a quaternary ammonium fluoride (e.g., Me4NF, Et4NF, n-Bu4NF, (PhCH2)4NF) exclusively substitutes the iodyl moiety in these derivatives and provides high specific activity F- 18 labeled fluoroaryl analogs. Iodyl derivatives of a benzothiazole analog and 6-iodyl-L-dopa derivatives have been synthesized as precursors and have been used in the preparation of no-carrier-added [F-18]fluorobenzothiazole as well as 6-[F-18]fluoro-L-dopa.