Radiolabelling Process
AssigneeGe Healthcare Limited
InventorTorild Wickstrom
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Abstract
The present invention relates to a novel composition comprising 1-amino-3[18F]-fluorocyclobutanecarboxylic acid ([18F]-FACBC) wherein said composition has certain superior properties in comparison with known compositions comprising [18F]-FACBC. Also provided by the invention is a method to obtain said composition.
Claims24
A method to obtain a composition comprising 1-amino-3-[18F]-fluorocyclobutanecarboxylic acid ([18F]-FACBC) wherein said composition comprises acetonitrile (MeCN) at a concentration of no greater than 50 μg/mL wherein said method comprises:
- reacting [18F]fluoride with a precursor compound of Formula I:
- wherein:
- LG is a leaving group;
- PG1 is carboxy protecting group;
- and,
- PG2 is an amine protecting group;
- wherein said reacting step is carried out in acetonitrile;
- to obtain a reaction mixture comprising a compound of Formula II:
- wherein:
- PG1 and PG2 are as defined for Formula I;
- transferring said compound of Formula II out of said reaction vessel to carry out removal of PG1 and thereby obtain a compound of Formula III:
- wherein PG2 is as defined for Formula I;
- simultaneously to step(ii) applying heat to said reaction vessel;
- and
- transferring said compound of Formula III back into said reaction vessel to carry out removal of PG2 and thereby obtain [18F]-FACBC.
A composition comprising 1-amino-3-[18F]-fluorocyclobutanecarboxylic acid (['18F]-FACBC) wherein said composition comprises acetonitrile (MeCN) at a concentration of no greater than 50 μg/mL.
Dependencies are inferred from the claim text.