NDLI: New fluorine-18 labeled benzaldehydes as precursors in the synthesis of radiopharmaceuticals for positron emission tomography

Content Provider	Springer Nature Link
Author	Orlovskaja, V. V. Fedorova, O. S. Studentsov, E. P. Golovina, A. A. Krasikova, R. N.
Copyright Year	2016
Abstract	4,5-Bis(butoxy)-2-nitrobenzaldehyde and 4,5-bis(tert-butoxycarbonyloxy)-2-nitrobenzaldehyde, as well as their fluorine-18 labeled derivatives (the half-life of F$^{18}$ is T $_{1/2}$ = 110 min) were synthesized for use as precursors in the synthesis of fluorine-18 labeled catecholamines and 6-[$^{18}$F]fluoro-l-DOPA ((S)-3-[4,5-dihydroxy-2-[$^{18}$F]fluorophenyl]-2-aminopropionic acid), important radiopharmaceutical agents (RPAs) for positron emission tomography. An advantageous feature of the newly obtained substituted nitrobenzaldehydes is the presence of labile protective groups which can be removed without using aggressive chemicals and severe conditions, which is of fundamental importance for automation of the RPA synthesis in modern synthesis apparatus. A high and stable radiofluorination yield achieved under the optimum fluorination conditions (Kryptofix 222 [K/K2.2.2.]$^{+}$[$^{18}$F$^{–}$], DMF, 140 °C, 10 min) using 4,5-bis(butoxy)-2-nitrobenzaldehyde as a substrate (83±6%, the number of experiments was n = 15) makes this compound a precursor of choice for the radioactive synthesis.
Starting Page	507
Ending Page	512
Page Count	6
File Format	PDF
ISSN	10665285
Journal	Russian Chemical Bulletin
Volume Number	65
Issue Number	2
e-ISSN	15739171
Language	English
Publisher	Springer US
Publisher Date	2016-11-08
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	fluorine-18 $^{18}$F radiopharmaceuticals positron emission tomography substituted nitrobenzaldehydes nucleophilic radiofluorination fluorine-18 labeled aromatic amino acids Chemistry/Food Science Organic Chemistry Inorganic Chemistry
Content Type	Text
Resource Type	Article
Subject	Chemistry

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