Premium
An improved enantioselective synthesis of no‐carrier‐added (NCA) 6‐[ 18 F]FLUORO‐L‐DOPA
Author(s) -
Wang Y. X.,
Zhang L.,
Tang G. H.,
Yin D. Z.
Publication year - 2001
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/jlcr.25804401304
Subject(s) - chemistry , trifluoromethanesulfonate , bromide , nucleophile , enantioselective synthesis , catalysis , electrophile , dopamine , high performance liquid chromatography , fluoride , chemical synthesis , medicinal chemistry , nuclear chemistry , organic chemistry , inorganic chemistry , neuroscience , biology , biochemistry , in vitro
6‐[ 18 F]Fluoro‐L‐Dopa (6‐FDOPA) is the analogue of L‐Dopa, the biosynthesis precursor for dopamine. As a PET tracer, it was widely applied for the presynaptic dopamine function in cerebral studies in humans. The synthesis routes to this radiopharmaceutical could be divided into two main groups, that is, electrophilic and nucleophilic route. Lemaire et al reported a new nucleophilic synthesis procedure using a chiral phase‐transfer catalyst. A similar procedure with some improvements was described in this study. A trimethylammonium veratraldehyde triflate was synthesized and used as a precurser for the synthesis of 6‐[ 18 F]Fluoro‐L‐Dopa by using the chiral phase‐transfer catalyst, O‐Allyl‐N‐(9)‐anthracenylcinchonidinium Bromide which was also synthesized in this study. The nca Fluorine‐ 18 F‐fluoride was produced by the 18 O(p, n) 18 F nuclear reaction on enriched water. First the 6‐[ 19 F]Fluoro‐L‐Dopa was synthesized to test the chemical structure of the synthesized end product and whole prcedure. Then the synthesis of 6‐[ 18 F]Fluoro‐L‐Dopa was completed and identified by HPLC, TLC and MS(only the case of the 6‐[ 19 F]Fluoro‐L‐Dopa).