914394-64-2

Upstream product

• 383-50-6 2-fluoroethyl tosylate 
• 121-33-5 vanillin 
• 762-49-2 2-fluoroethyl bromide 
• 99070-23-2 4-(2-bromo-ethoxy)-3-methoxy-benzaldehyde 
• 17792-74-4 4-methylbenzenesulfonic acid [(4-formyl-2-methoxyphenoxy)ethyl] ester 

Downstream Products

• 1012885-00-5 C₂₀H₂₄ClFN₂O₂ 
• 1012884-92-2 C₂₁H₂₇FN₂O₃ 
• 1338227-30-7 (1E,4Z,6E)-1-(3,4-dimethoxyphenyl)-7-(4-(2-fluoroethoxy)-3-methoxyphenyl)-5-hydroxy-hepta-1,4,6-trien-3-one 
• 1335093-75-8 2-(3-fluoro-4-methoxyphenyl)-N-(2-(4-(2-fluoroethoxy)-3-methoxyphenyl)-2-methoxyethyl)acetamide 
• 1335093-76-9 N-(2-(4-(2-fluoroethoxy)-3-methoxyphenyl)-2-methoxyethyl)-2-(4-methoxy-3-methylphenyl)acetamide 
• 1335093-77-0 N-(2-(4-(2-fluoroethoxy)-3-methoxyphenyl)-2-methoxyethyl)-2-(4-(methylthio)phenyl)acetamide 
• 1335093-78-1 2-(2-fluoro-4-methoxyphenyl)-N-(2-(4-(2-fluoroethoxy)-3-methoxyphenyl)-2-methoxyethyl)acetamide 
• 1335093-79-2 2-(5-bromo-2-methoxyphenyl)-N-(2-(4-(2-fluoroethoxy)-3-methoxyphenyl)-2-methoxyethyl)acetamide 
• 1335093-80-5 2-(3-bromo-4-methoxyphenyl)-N-(2-(4-(2-fluoroethoxy)-3-methoxyphenyl)-2-methoxyethyl)acetamide 
• 1335093-81-6 N-(2-(4-(2-fluoroethoxy)-3-methoxyphenyl)-2-methoxyethyl)-2-(3-fluorophenyl)acetamide 
• 1335093-82-7 N-(2-(4-(2-fluoroethoxy)-3-methoxyphenyl)-2-methoxyethyl)-2-(3-(2-fluoroethoxy)-4-methoxyphenyl)acetamide 
• 1335093-83-8 2-(3,5-dimethoxyphenyl)-N-(2-(4-(2-fluoroethoxy)-3-methoxyphenyl)-2-methoxyethyl)acetamide 
• 1335093-84-9 2-(4-fluoro-3-methoxyphenyl)-N-(2-(4-(2-fluoroethoxy)-3-methoxyphenyl)-2-methoxyethyl)acetamide 
• 1335093-86-1 2-(4-(benzyloxy)-3-methoxyphenyl)-N-(2-(4-(2-fluoroethoxy)-3-methoxyphenyl)-2-methoxyethyl)acetamide 

Relevant academic research and scientific papers

Synthesis and characterization of 18F-labeled hydrazinocurcumin derivatives for tumor imaging

Fluorine-substituted hydrazinocurcumin derivative 1 and its dimethyl-substituted form at the C2 and C6 positions (2) were synthesized and their radiolabeled forms, [18F]1 and [18F]2, were evaluated for tumor imaging. In vitro and in vivo metabolism studies showed that the two radioligands were resistant to reductive metabolism, probably due to the presence of a pyrazole ring. In cellular uptake studies, [18F]1 and [18F]2 exhibited comparable uptake by human umbilical vascular endothelial cells and rat C6 glioma cells. Inhibition of radioligand uptake to a similar extent by HC and curcumin suggests that these radioligands may share the same binding sites as those for HC and curcumin. Positron emission tomography imaging of C6 glioma xenografted mice acquired 30 and 60 min after radioligand injection showed that [18F]2 had markedly higher tumor uptake than [18F]1, which was consistent with biodistribution data (3.20 ± 0.35% ID per g vs. 0.98 ± 0.31% ID per g, respectively). However, the two radioligands showed similar levels of tumor-to-background uptake ratio, except for the significantly higher uptake of [18F]1 by the small intestine, indicating its more rapid clearance. The results of this study will guide further structural modifications of these radioligands to enhance tumor-to-background uptake ratios.

Synthesis and evaluation of 1-(4-[18F]fluoroethyl)-7-(4′- methyl)curcumin with improved brain permeability for β-amyloid plaque imaging

Alzheimer's disease is characterized by the accumulation of β-amyloid (Aβ) plaques and neurofibrillary tangles (NFTs) in the brain. We previously developed [18F]fluoropropylcurcumin ([18F]FP-curcumin), which demonstrated excellent bi

Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A

A series of analogues were synthesized by optimizing the structure of papaverine. The in vitro PDE10A binding affinity (IC50) values for these new analogues were measured; for compounds that have IC50 value less than 60 nM for PDE10A

Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker

Employing D4 selective azaindoles as lead compounds, a focused library of the carbocyclic arene bioisosteres 1 was synthesized when we took advantage of the click chemistry derived triazolylmethyl acrylate resin 2. Ligand binding assays on monoaminergic GPCRs led to SARs that indicated further lead structure optimizations when the attachment of alkoxy substituents provided both an improvement of the biological properties and the opportunity to introduce 18F as a radioisotope. Finally, radiosynthesis resulted in formation of the radioligand [18F]7h that showed optimal log D7.4 of 2.8 and was determined to be highly stable in human serum. Thus, [18F]7h represents a promising dopamine D4 selective radioligand for positron emission tomography (PET).

IMIDAZOL [1,2-A] PYRIDINES AND RELATED COMPOUNDS WITH ACTIVITY AT CANNABINOID CB2 RECEPTORS

Disclosed are compounds of Formula (I) or Formula (II) or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof; and methods of modulating the activity of a cannabinoid CB2 receptor comprising contacting a compound of Formula (I) or Formula (II) with the cannabinoid CB2 receptor. Said compounds are useful in the treatment of various condition and disorders such as pain, and neurodegenerative disorders.

Curcumin and dehydrozingerone derivatives: Synthesis, radiolabeling, and evaluation for β-amyloid plaque imaging

Alzheimer's disease (AD) is pathologically characterized by the accumulation of amyloid plaques and neurofibrillary tangles in the brain, and thus, the in vivo imaging of plaques and tangles would be beneficial for the early diagnosis of AD. It has been s