50370-59-7

Upstream product

• 352-13-6 4-flourophenylmagnesium bromide 
• 50373-10-9 methyl ecgonidine 
• 201472-98-2 (1S)-N-methyl-2-carbomethoxy-3-{[(trifluoromethyl)sulfonyl]oxy}-8-azabicyclo[3.2.1]-2-octene 
• 112652-64-9 (S)-(-)-2-(carbomethoxy)-3-tropinone 
• 201472-99-3 (1S)-N-methyl-2-carbomethoxy-3-(4-fluorophenyl)-8-azabicyclo[3.2.1]-2-octene 
• 50373-10-9 (1S)-anhydroecgonine methyl ester 
• 53-21-4 (-)-cocaine hydrochloride 
• 5796-31-6 ecgonine hydrochloride 
• 53757-87-2 (1R,2S,5R)-8-Methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester 
• 481-37-8 ecgonine 
• 484-93-5 ecgonidine 
• 50-36-2 Cocaine 
• 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 

Downstream Products

• 50370-57-5 O-1492 
• 208989-00-8 (1R,5S)-3β-(p-fluorophenyl)-2β-formyltropane 
• 201472-89-1 (1S,2R,3R,5R)-2-(Benzo[1,3]dioxol-5-yloxymethyl)-3-(4-fluoro-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane 
• 201472-83-5 (1S)-2β-hydroxymethyl-3β-(4-fluorophenyl)tropane 
• 131488-15-8 2β-Carbomethoxy-3β-(4-fluorophenyl)-8-azabicyclo[3.2.1]octane 
• 127627-50-3 2β-carbomethoxy-3β-(4-fluorophenyl)-8-propylnortropane 
• 127648-29-7 2β-carbomethoxy-3β-(4-fluorophenyl)-8-allylnortropane 
• 201472-86-8 (1R,2S,3S,5S)-2-(Benzo[1,3]dioxol-5-yloxymethyl)-3-(4-fluoro-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane 
• 217438-61-4 2β-<(4,7-dithiaoctanoyloxy)methyl>-3β-(4-fluorophenyl)tropane 
• 263841-48-1 (1R,2S,3S,5S)-8-Ethoxycarbonylmethyl-3-(4-fluoro-phenyl)-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester 
• 306740-58-9 N-[2-(3'-N'-propyl-(1''R)-3''β-(4-fluorophenyl)tropane-2''β-(1-propanoyl))((2-((triphenylmethyl)thio)ethyl)amino)acetyl]-S-(triphenyl)-2-aminoethanethiol 
• 306740-53-4 2β-carboxylic acid methoxymethylamide-3β-(4-fluorophenyl)-8-methyl-8-azabicyclo[3.2.1]octane 
• 306740-56-7 2β-(1-propanoyl)-3β-(4-fluorophenyl)-8-azabicyclo[3.2.1]octane 

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.

BOLAAMPHIPHILIC COMPOUNDS, COMPOSITIONS AND USES THEREOF

Bolaamphiphilic compounds are provided according to formula (I): where HG1, HG2 and L1 are as defined herein. Provided bolaamphilphilic compounds and the pharmaceutical compositions thereof are useful for delivering GDNF or NGF into animal or human brain.

Synthesis and monoamine uptake inhibition of conformationally constrained 2β-carbomethoxy-3β-phenyl tropanes

A series of 2β-carbomethoxy-3β-phenyl tropanes with conformationally constrained nitrogen substituents were synthesized as potential selective dopamine transporter ligands. These novel compounds were examined for their monoamine uptake inhibition potency at the human dopamine transporter (hDAT), the human serotonin transporter (hSERT) and the human noradrenalin transporter (hNET), stably expressed in human embryonic kidney cells (HEK). A SAR-study was conducted to determine the contribution of extended, 4-fluorinated, conformationally constrained C4 chains at the tropane nitrogen to human monoamine transporter affinity and selectivity. The Royal Society of Chemistry 2009.

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

Tropane derivatives and method for their synthesis

A compound of formula (I) wherein R1-R6have any of the values defined in the specification are described, as well as pharmaceutical compositions comprising a compound of formula (I), and methods for preparing and using compounds of f

Fluoralkenyl nortropanes

Provided are compounds of the following formula: wherein R is C2-C6 mono- or multi-unsaturated hydrocarbon having one or more ethylene, acetylene or allene groups, A is 18 or 19, and X is H or halogen. The compounds of the invention bind to dopamine transporter with high affinity and selectivity and are thus useful as diagnostic and therapeutic agents for diseases associated with dopamine transporter dysfunction. The radiolabeled compounds are useful as imaging agents for visualizing the location and density of dopamine transporter by PET imaging.

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.

Tropane-derivatives, their preparation and use

Compounds of formula (a), (b), (c), or (d), or any mixture thereof, or a pharmaceutically-acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R3 is —CH2—X—R′, wherei

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.

Design, synthesis and biological evaluation of 7-azatricyclodecanes: Analogues of cocaine

The synthesis and biological activity of a series of azatricyclodecane analogues of cocaine are described. All compounds studied in this series exhibit nanomolar potency and good selectivity for the serotonin transporter versus the dopamine transporter. (