174224-35-2

Upstream product

• 50373-10-9 methyl ecgonidine 
• 17878-43-2 [4-(trimethylsilyl)phenyl]magnesium bromide 
• 6999-03-7 1-bromo-4-(trimethylsilyl)benzene 
• 53757-87-2 (1R,2S,5R)-8-Methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester 

Downstream Products

• 303731-40-0 (1R,2S,3S,5S)-3-[4-(3-Hydroxy-propyl)-phenyl]-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester 
• 303731-39-7 (1R,2S,3S,5S)-3-[4-(2-Hydroxy-ethyl)-phenyl]-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester 
• 181796-40-7 3β-(4'-allylphenyl)tropane-2β-carboxylic acid methyl ester 
• 181796-42-9 3β-(4'-vinylphenyl)tropane-2β-carboxylic acid methyl ester 
• 398497-75-1 (1R,2S,3S,5S)-3-(4-Iodo-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid 3-methanesulfonyloxy-propyl ester 
• 398497-81-9 (1R,2S,3S,5S)-2-fluoroethyl 3-(4-iodophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate 
• 189950-17-2 Nor-CBT 
• 172651-49-9 N-3-fluoropropyl-3-β-(4-iodophenyl)nortropane-2-β-carboxylic acid 
• 155797-99-2 FP-beta-CIT 
• 141807-58-1 RTI 102 
• 180057-11-8 (1R,2S,3S,5S)-3-(4-Iodo-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carbonyl chloride 
• 136794-87-1 (1R,2S,3S,5S)-3-(4-Iodo-phenyl)-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester 
• 135416-43-2 (1R,2S,3S,5S)-3-(4-Iodo-phenyl)-8-methyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester 
• 135367-08-7 RTI 51 

Relevant academic research and scientific papers

PROCESS FOR THE PREPARATION OF RADIOIODINATED 3-FLUOROPROPYL-NOR-Beta-CIT

The invention generally provides processes for the preparation of radioiodinated 3-fluoropropyl-nor-β-CIT. In particular, the process uses an arylsilane intermediate, thus avoiding the use of hexamethylditin, and reducing the number of steps previously required for the preparation of radioiodinated 3-fluoropropyl-nor-β-CIT from anhydroecgonine methyl ester. The invention also relates to the alkylation of a nortropane to the corresponding N-(3-fluoropropyl) analogue using 3-fluoropropanal.

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.

Synthesis and biological evaluation of a series of novel N- or O-fluoroalkyl derivatives of tropane: Potential positron emission tomography (PET) imaging agents for the dopamine transporter

A series of novel fluoroalkyl-containing tropane derivatives was synthesized, and their binding affinities for the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET) were determined via competitive binding assays. Among these derivatives, the fluoropropyl ester of β-CIT (19), the fluoroethyl ester of β-CIT (20), the N-fluoropropyl derivative of β-CBT (12), and the fluoropropyl ester of β-CMT (18) displayed higher affinity and greater selectivity for the DAT versus SERT and NET than FP-CIT, which indicates that they are attractive candidates for the development of 18F-labeled PET imaging agents for the DAT.