373604-75-2

Upstream product

• 148319-23-7 (+/-)-1-(2-hydroxyethyl)-3-piperidinecarboxylic acid ethyl ester 
• 373604-74-1 2-(4-(bis(4-methoxyphenyl)chloromethyl)phenoxy)ethyl acetate 
• 71962-74-8 Ethyl nipecotate 
• 373604-73-0 2-(4-(bis(4-methoxyphenyl)hydroxymethyl)phenoxy)ethan-1-ol 

Downstream Products

• 373604-76-3 1-{2-[[4-(2-hydroxy-ethoxy)-phenyl]-bis-(4-methoxy-phenyl)-methoxy]-ethyl}-piperidine-3-carboxylic acid ethyl ester 
• 373604-77-4 1-[2-(bis-(4-methoxy-phenyl)-{4-[2-(toluene-4-sulfonyloxy)-ethoxy]-phenyl}-methoxy)-ethyl]-piperidine-3-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

Radiosynthesis of (±)-(2-((4-(2-[18F]fluoroethoxy)phenyl)bis(4-methoxy- phenyl) methoxy)ethylpiperidine-3-carboxylic acid: A potential GAT-3 PET ligand to study GABAergic neuro-transmission in vivo

A dysfunction of GABAergic neurotransmission is related to diseases such as epilepsy, Huntington-disease and Parkinson-syndrome. A new 18F-fluorine labelled GABA transporter ligand for the GABA-transporter subtype GAT-3 was developed which may allow the in vivo visualisation of GABAergic neurotransmission. The precursors ethyl (2-(4-hydroxyphenyl)bis (4-methoxyphenyl)-methoxy)ethyl)-piperidine-3-carboxylate and ethyl(2-((4-(2-tosylethoxy)phenyl)-bis(4-methoxyphenyl)-methoxy) ethyl)piperidine-3-carboxylate were synthesised and labelled by the use of 2-[18F]fluoroethyltosylate or [18F]fluoride. Subsequent cleavage of the ester moiety gave the final product (±)-(2-((4-(2-[18F]fluoroethoxy)phenyl)bis(4-methoxy- phenyl)methoxy)ethyl)-piperidine-3-carboxylic acid in a decay corrected yield of 33-36%. Preliminary biodistribution kinetics were determined with BALB/c mice ex vivo for brain, liver, kidney, spleen, blood and bone. (2-((4-(2-[18F]fluoroethoxy)-phenyl)bis(4-methoxyphenyl)methoxy)- ethyl) piperidine-3-carboxylic acid showed a maximum brain uptake after 1 h p.i. of about 0.3% ID/g. Copyright