86656-36-2

Upstream product

• 552-89-6 2-nitro-benzaldehyde 
• 89-98-5 2-chloro-benzaldehyde 
• 446-52-6 2-Fluorobenzaldehyde 
• 6630-33-7 ortho-bromobenzaldehyde 
• 131948-17-9 2-formyl-N,N,N-trimethylbenzenaminium triflate 
• 380151-85-9 2-(2'-formylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane 
• 529-23-7 o-aminobenzaldehyde 
• 40138-16-7 2-formylbenzene boronic acid 

Downstream Products

• 134430-68-5 C₇H₇⁽¹⁸⁾FO 
• 133629-91-1 C₇H₆Cl⁽¹⁸⁾F 
• 134430-69-6 2-⁽¹⁸⁾fluorobenzyl bromide 
• 134430-71-0 C₇H₆⁽¹⁸⁾FI 
• 159979-96-1 4-fluorobenzyl azide 

Relevant academic research and scientific papers

Exploration of alcohol-enhanced Cu-mediated radiofluorination toward practical labeling

Copper-mediated nucleophilic radiofluorination using boronic precursors is a promising, general method to label aromatic compounds with [18F]fluoride. However, in various reports, large amounts of precursor (60 μmol) were needed to achieve high

Molecular Imaging of Sirtuin1 Expression-Activity in Rat Brain Using Positron-Emission Tomography-Magnetic-Resonance Imaging with [18F]-2-Fluorobenzoylaminohexanoicanilide

Sirtuin 1 (SIRT1) is a class III histone deacetylase that plays significant roles in the regulation of lifespan, metabolism, memory, and circadian rhythms and in the mechanisms of many diseases. However, methods of monitoring the pharmacodynamics of SIRT1

Synthesis, radiofluorination, and preliminary evaluation of the potential 5-HT2A receptor agonists [18F]Cimbi-92 and [18F]Cimbi-150

An agonist PET tracer is of key interest for the imaging of the 5-HT2A receptor, as exemplified by the previously reported success of [11C]Cimbi-36. Fluorine-18 holds several advantages over carbon-11, making it the radionuclide of choice for clinical purposes. In this respect, an 18F-labelled agonist 5-HT2A receptor (5-HT2AR) tracer is highly sought after. Herein, we report a 2-step, 1-pot labelling methodology of 2 tracer candidates. Both ligands display high in vitro affinities for the 5-HT2AR. The compounds were synthesised from easily accessible labelling precursors, and radiolabelled in acceptable radiochemical yields, sufficient for in vivo studies in domestic pigs. PET images partially conformed to the expected brain distribution of the 5-HT2AR; a notable exception however being significant uptake in the striatum and thalamus. Additionally, a within-scan displacement challenge with a 5-HT2AR antagonist was unsuccessful, indicating that the tracers cannot be considered optimal for neuroimaging of the 5-HT2AR.

RADIOFLUORINATED 7-AMINO-5-THIO-THIAZOLO[4,5-D]PYRIMIDINES FOR IMAGING FRACTALKINE RECEPTOR (CX3CR1)

Radiofluorinated 7-Amino-5-thio-thiazolo[4,5-d]pyrimidines targeting Fractalkine Receptor (CX3CR1) are disclosed. Methods of imaging CX3CR1-expressing tumors or cells also are disclosed.

Neither azeotropic drying, nor base nor other additives: A minimalist approach to 18F-labeling

A novel, efficient, time-saving and reliable radiolabeling procedure via nucleophilic substitution with [18F]fluoride is described. Different radiolabeled aliphatic and aromatic compounds were prepared in high radiochemical yields simply by hea

Fast and reliable method for the preparation of ortho- and para-[ 18F]fluorobenzyl halide derivatives: Key intermediates for the preparation of no-carrier-added PET aromatic radiopharmaceuticals

A fast and reliable method suitable for the automated preparation of (substituted) [18F]fluorobenzyl halides from several [ 18F]fluorobenzaldehydes was developed. Aromatic nucleophilic substitution of trimethylammonium benzaldehyde t

Nucleophilic [18F]Fluorination and subsequent decarbonylation of methoxy-substituted nitro- and halogen-benzenes activated by one or two formyl groups

As model reactions for the introduction of 18F into protected aromatic amino acids, the replacement of NO2, Cl, Br and F by [ 18F]fluoride in 2-isophthalaldehyde and 2-terephthalaldehyde derivatives which model 18/su

Nucleophilic substitution of nitro groups by [18F]fluoride in methoxy-substituted ortho-nitrobenzaldehydes-A systematic study

As model reactions for the introduction of [18F]fluorine into aromatic amino acids, the replacement of NO2 by [18F]fluoride ion in mono- to tetra-methoxy-substituted ortho-nitrobenzaldehydes was systematically investigated. Unexpectedly, the highly methoxylated precursors 2,3,4-trimethoxy-6-nitrobenzaldehyde and 2,3,4,5-tetramethoxy-6-nitrobenzaldehyde showed high maximum radiochemical yields (82% and 48% respectively). When the electrophilicity of the leaving group substituted carbon atom is expressed by its 13C NMR chemical shift a good correlation with the reaction rate at the beginning of the reaction (first min) was found (R2 = 0.89), whereas the maximum radiochemical yields correlated much poorer with this electrophilicity parameter. This may be caused by side reactions becoming influencial in the further reaction course. As possible side reactions the demethylation of methoxy groups and intramolecular redox reactions could be detected by HPLC/MS.

Effect of aldehyde and methoxy substituents on nucleophilic aromatic substitution by [18F]fluoride

For a series of benzaldehydes only with a leaving group or with both a leaving group and a single methoxy substituent 18F-fluorination via nucleophilic aromatic substitution (SNAr) was studied in DMF and Me2SO. In general, the radiochemical yields were clearly higher in DMF than in Me2SO. In the fluorodehalogenation reaction (leaving group: halogen = Br, Cl), extremely low radiochemical yields were observed in Me2SO (2SO (within 3 min reaction time, 90% of the precursor was consumed; radiochemical yield = 1.0 ± 0.5%); however, in DMF oxidation was always kept at a low level during the entire reaction (13C-NMR ppm values of the aromatic carbon atom bearing the leaving group.

2-Amino-2'-[18F]fluorobenzhydrols, intermediates for the synthesis of [2'-18F]-1,4-benzodiazepine-2-ones

A method for synthesizing 18F-labelled 2-amino-2'-fluorobenzhydrols under no-carrier-added conditions for use as radiolabelled intermediates in the synthesis of [2'-18F]-1,4-benzodiazepine-2-ones is presented. Anilinodichloroborane r