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Synthesis of [ 18 F]Ro41‐0960, a potent catechol‐O‐methyltransferase inhibitor, for PET studies
Author(s) -
Ding Y.S.,
Sugano Y.,
Koomen J.,
Aggarwal D.
Publication year - 1997
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(199704)39:4<303::aid-jlcr977>3.0.co;2-w
Subject(s) - chemistry , nucleophilic substitution , nucleophilic aromatic substitution , catechol , nucleophile , nitro , hydrolysis , catechol o methyl transferase , medicinal chemistry , stereochemistry , organic chemistry , biochemistry , alkyl , allele , gene , catalysis
Ro41‐0960 (3,4‐dihydroxy‐5‐nitro‐2′‐fluorobenzophenone) is a potent, fluorine containing COMT inhibitor. In order to map catechol‐O‐methyltransferase (COMT) in vivo with PET, no‐carrier‐added [ 18 F]Ro41‐0960 was synthesized by the nucleophilic aromatic substitution of [ 18 F]fluoride for 2′‐nitro on 3,4‐dimethoxy‐5,2′‐dinitrobenzophenone, followed by hydrolysis with HBr. During the course of this study it was found that [ 18 F]fluoromethane ([ 18 F]CH 3 F) was generated as the side product of nucleophilic aromatic substitution reaction. Various precursors with different hydroxyl protecting groups were then investigated for the effects on this side reaction. © 1997 John Wiley & Sons, Ltd.