956103-76-7

Basic information

• Product Name: Florbetapir F 18
• Synonyms: Florbetapir F 18;18F-AV45;Florbetapir (18F);AV-45 compound;4-[(E)-2-[6-[2-[2-(2-fluoranylethoxy)ethoxy]ethoxy]pyridin-3-yl]ethenyl]-N-methylaniline
• CAS NO: 956103-76-7
• Molecular Formula: C₂₀H₂₅FN₂O₃
• Molecular Weight: 360.4225032
• Mol File: 956103-76-7.mol
• Article Data: 5

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Florbetapir F 18(CAS DataBase Reference)
• NIST Chemistry Reference: Florbetapir F 18(956103-76-7)
• EPA Substance Registry System: Florbetapir F 18(956103-76-7)

Safety Data

• Hazardous Substances Data: 956103-76-7(Hazardous Substances Data)

Usage

Definition

ChEBI: An aromatic ether consisting of a pyridine ring substituted at position 2 by a 2-{2-[2-(18F)fluoroethoxy]ethoxy}ethoxy group and at position 5 and a 2-(4-methylaminophenyl)vinyl group. A positron emission tomography imaging ligand for he detection of amyloid aggregation associated with Alzheimer disease.

Upstream product

• 1205550-99-7 (E)-2-[2-[2-[5-[4-[tert-butoxycarbonyl[methyl]amino]styryl]pyridine-2-yloxy]ethoxy]ethoxy]ethyl 4-methylbenzenesulfonate 

Relevant articles and documents

Preparation and stability of ethanol-free solution of [18F] florbetapir ([18F]AV-45) for positron emission tomography amyloid imaging

We have developed an ethanol-free formulation method of [ 18F]florbetapir ([18F]AV-45) using a commercially available automated JFE multi-purpose synthesizer. We have also evaluated the radiochemical stability in an ethanol-free solution of [ 18F]AV-45 under visible light irradiation and dark conditions by comparison with a conventional 10% ethanol solution of [18F]AV-45. [18F]AV-45 was obtained with a radiochemical yield of 55.1 ± 2.2% (decay-corrected to end of bombardment), specific activity of 591.6 ± 90.3 GBq/μmol and radiochemical purity of >99% within a total synthesis time of about 73 min. The radiochemical purity of [ 18F]AV-45 formulated by dissolving the ethanol-free solution was found to decrease as a function of the period of exposure to visible light. In contrast, the visible light photolysis could be suppressed by adding 10% ethanol to the formulation or by avoiding exposure to visible light. In the radiosynthesis of [18F]AV-45 formulated by dissolving the ethanol-free solution, [18F]AV-45 could be obtained with high radiochemical purity and high stability by avoiding exposure to visible light. Copyright

A New Highly Deuterated [18F]AV-45, [18F]D15FSP, for Imaging β-Amyloid Plaques in the Brain

[18F]AV-45 (florbetapir f18, Amyvid) is an FDA-approved PET imaging agent targeting Aβ plaques in the brain for diagnosis of Alzheimer's disease (AD). Its metabolites led to a high background in the brain and large bone uptake of [18F]F-, produced from dealkylation of the PEG chain. To slow down the in vivo metabolism, we report the design, synthesis, and evaluation of a highly deuterated derivative, [18F]D15FSP, and compared it with N-methyl-deuterated [18F]D3FSP and nondeuterated [18F]AV-45. D15FSP displayed excellent binding affinity (Ki = 7.52 nM) to Aβ aggregates. In vitro autoradiography of [18F]D15FSP, [18F]D3FSP, and [18F]AV-45 showed excellent binding to Aβ plaques in human AD brain sections. Biodistribution studies displayed lower bone uptake at 120 min for [18F]D15FSP compared to that for [18F]D3FSP and [18F]AV-45 (1.44 vs 4.23 and 4.03%ID/g, respectively). As the highly deuterated [18F]D15FSP displayed excellent Aβ binding affinity, high initial brain penetration, and lower bone retention, it might be suitable for PET imaging in detecting Aβ plaques.

METHOD FOR PREPARING FLUORINE-18 ELUENT WITH ADJUSTED PH, AND METHOD FOR LABELLING FLUORINE-18 USING SAME

The present invention relates to a method for labelling fluorine-18, which is a radioisotope, and more specifically, to a method for labelling a [18F]fluoride in a method for preparing an organic [18F]fluoro compound by reacting an a