157008-48-5

Upstream product

• 67-56-1 methanol 
• 184376-51-0 (1R,2R,3R,5S)-3-(4-Fluoro-phenyl)-8-methyl-2-(3-methyl-[1,2,4]oxadiazol-5-yl)-8-aza-bicyclo[3.2.1]octane 
• 5796-31-6 ecgonine hydrochloride 
• 53-21-4 (-)-cocaine hydrochloride 
• 168143-65-5 methyl (1R,5S)-8-methyl-3-(((trifluoromethyl)sulfonyl)oxy)-8-azabicyclo[3.2.1]oct-2-ene-2-carboxylate 
• 85506-18-9 (1R)-(-)-2-carbomethoxy-3-tropinone 
• 352-13-6 4-flourophenylmagnesium bromide 
• 50373-10-9 methyl ecgonidine 
• 168254-92-0 (1R,2S,3R,5S)-(p-fluorophenyl)-2-(3'-methyl-1',2',4-oxadiazol-5'-yl)tropane 
• 168143-68-8 O-1104 

Downstream Products

• 201472-82-4 [(1R,2S,3R,5S)-3-(4-Fluoro-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]oct-2-yl]-methanol 
• 306740-63-6 (1R)-2β-carboxylic acid methoxymethylamide-3α-(4-fluorophenyl)-8-methyl-8-azabicyclo[3.2.1]octane 
• 306740-94-3 (1R)-2β-methoxycarbonyl-3α-(4-fluorophenyl)-8-azabicyclo[3.2.1]-octane 
• 306740-65-8 (1R)-2β-(1-propanoyl)-3α-(4-fluorophenyl)-8-methyl-8-azabicyclo[3.2.1]octane 
• 306740-67-0 (1R)-2β-(1-propanoyl)-3α-(4-fluorophenyl)-8-azabicyclo[3.2.1]octane 
• 306740-69-2 N-[2-(3'-N'-propyl-(1''R)-3''α-(4-fluorophenyl)tropane-2''β-(1-propanoyl))((2-((triphenylmethyl)thio)ethyl)amino)acetyl]-S-(triphenyl)-2-aminoethanethiol 
• 201472-88-0 (1R,2S,3R,5S)-2-(Benzo[1,3]dioxol-5-yloxymethyl)-3-(4-fluoro-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane 
• 850888-35-6 (1R)-2β-[(3,4-methylenedioxy)phenoxy]methyl-3α-(4-fluorophenyl)-8-(4-methyl benzenesulfonyl)tropane 
• 850888-33-4 (1R)-2β-carbomethoxy-3α-(4-fluorophenyl)-8-(4-methyl benzenesulfonyl)tropane 
• 850888-34-5 (1R)-2β-hydroxymethyl-3α-(4-fluorophenyl)-8-(4-methyl benzenesulfonyl)tropane 

Relevant academic research and scientific papers

Copper-mediated nucleophilic radiofluorination of [18F]β-CFT for positron emission tomography imaging of dopamine transporter

[18F]β-CFT is a positron emission tomography (PET) ligand for imaging of dopamine transporter. It was proved to be a sensitive PET marker to detect presynaptic dopaminergic hypofunction in Parkinson's disease. In recent years, copper-mediated 18F-fluorination of aryl boronic esters has been successful in some molecules containing aromatic groups. In this study, we describe the novel synthetic strategy of [18F]β-CFT by copper-mediated nucleophilic radiofluorination with pinacol-derived aryl boronic esters upon reaction with [18F]KF/K222 and Cu (OTf)2(py)4. The radiolabeling protocol was optimized with [18F]fluoride elution method and amount of copper catalyst used. [18F]β-CFT is obtained from boronic ester precursors in 2.2% to 10.6% non-isolated radiochemical yield (RCY). Purified [18F]β-CFT with >99% radiochemical purity (RCP) and high molar activity was obtained in validation runs. The radiolabeling procedure is straightforward and can easily be adapted for clinical use.

A second-generation 99mtechnetium single photon emission computed tomography agent that provides in vivo images of the dopamine transporter in primate brain

The dopamine transporter (DAT), located presynaptically on dopamine neurons, provides a marker for Parkinson's disease (Pd) and attention deficit hyperactivity disorder (ADHD). In ADHD, DAT density levels are elevated, while in Pd these levels are deplete

Intermediates for the synthesis of radiolabelled tropanes

The compounds of the present invention comprise a tropane compound or ligand that selectively binds to tropane recognition sites, e.g., neuron transporters such as that DAT. The tropane ligand is radiolabeled with a radioactive technetium or rhenium by a chelating ligand which is attached to the tropane ligand by a linker. Tropane compounds or ligands useful in the pratice of the present invention can generally be represented by formula II where R1 and R2 are defined as above and where R1 can also be substituted at the C4 position of the tropane ring: Any tropane compound of the general formula II is useful in the present invention so long as it binds to DAT. Useful tropane analogs have a 3α-group,i.e., are of the boat configuration. Intermediates for the synthesis of the radiolabeled tropanes are claimed.

Synthesis and binding affinities of 2β-(3-iodoallyloxycarbonyl)-3β-(4-substituted-aryl)tropane analogues as ligands for the dopamine transporter studies

Tropane analogues from cocaine, which is known to be one of the most reinforcing and addictive compounds, were designed, synthesized, and characterized for inhibition of presynaptic uptake of dopamine (DA) in brain. Eight new derivatives of 3β-aryl-2β-(3-iodoallyloxycarbonyl)tropanes were synthesized and tested for their potential abilities to displace [3H]2β-carbomethoxy-3β-(4-fluorophenyl)tropane (WIN 35,428) binding to the rat striatal membranes.

Synthesis and ligand binding of tropane ring analogues of paroxetine

(3S,4R)-4-(4-Fluoropheny)-3-[[3,4- (methylenedioxy)phenoxy]methyl]piperidine [(3S,9R)-3, paroxetine] is a selective serotonin reuptake inhibitor (SSRI) used as an antidepressant in humans. In previous studies, we reported that certain (1R)-3β-(substituted

Synthesis of the 2β,3α- and 2β,3β-Isomers of 3-(p-substituted phenyl)tropane-2-carboxylic Acid Methyl Esters

The synthesis of 3-(p-substituted phenyl)trop-2-ene-2-carboxylic acid methyl ester 8 and its reduction with samarium iodide provide a new synthesis of 3β-(4'-substituted phenyl)tropane-2β-carboxylic acid methyl ester (2) and, in addition, give the first s