Automated radiosynthesis
AssigneeGe Healthcare Limited
InventorsJohn Woodcraft, L Clare Jones, Alessandra Gaeta, John William Trigg, Alexander Paul Jones, Stuart Plant, Alexander Jackson
Life of this patent
Estimating the term…
Abstract
The present invention provides a method to obtain radiofluorinated compounds useful for in vivo imaging GABAA receptors. The method of the invention is high-yielding and may conveniently be carried out on an automated synthesizer such as Fastlab™. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention. Novel precursor compounds useful in the method of the invention are also provided, as are a number of novel compounds obtained by the method of the invention.
Claims11
A method to obtain a compound of Formula I:
- wherein:
- R1 is hydrogen and R2 is 18F;
- and,
- R3 is a C3-5 heterocycle;
- or, R3 is C(═O)—O—R4 wherein R4 is hydrogen, or a straight- or branched-chain C1-4 alkyl;
- wherein said method comprises:
- (i) providing a precursor compound of Formula Ia:
- wherein:
- R11 is hydrogen and R12 is a leaving group selected from nitro, tri-C1-3 alkyl ammonium or —I+—Ar, wherein Ar is phenyl substituted with one or more R* groups, wherein R* is selected from hydrogen, nitro, cyano, halogen, C2-10 carboxyalkyl, C1-10 alkyl, C2-10 alkoxyalkyl, C1-10 hydroxyalkyl, C1-10 aminoalkyl, C1-10 haloalkyl, C6-14 aryl, C3-12 heteroaryl, C3-20 alkylaryl, C2-10 alkenyl, and C2-10 alkynyl;
- and,
- R13 is as defined for R3 of Formula I;
- and,
- (ii) reacting said precursor compound with a suitable source of [18F]Fluoride.
A compound of Formula I
- wherein R1 is hydrogen, R2 is 18F, R3 is —C(═O)—O—R4, wherein R4 is ethyl, isopropyl or tert-butyl.
Dependencies are inferred from the claim text.