# US 2023/0068052 A1 · Eluent solution

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- Number: US 2023/0068052 A1
- Document ID: US20230068052A1
- Status: Published application
- Kind: A1
- Application number: 17/962,686
- Filed: 2022-10-10
- Published: 2023-03-02
- Earliest claimed: 2010-12-29
- Assignees: Ge Healthcare Limited
- Applicants: Ge Healthcare Limited
- Inventors: Torild Wickstrom; Anders Svadberg; Ole Kristian Hjelstuen; Dag M. Evje; Liane Ochsenfeld
- Web page: https://patentgrep.com/patent/US20230068052A1

## CPC

- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 51/0406: {Amines, polyamines, e.g. spermine, spermidine, amino acids, (bis)guanidines}
- B01J 19/00: Chemical, physical or physico-chemical processes in general; Their relevant apparatus
- C01B 9/08: Fluorides
- C07B 59/00: Introduction of isotopes of elements into organic compounds {; Labelled organic compounds per se}
- C07B 59/001: {Acyclic or carbocyclic compounds}
- C07C 51/363: by introduction of halogen; by substitution of halogen atoms by other halogen atoms
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- B01J: CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- C01B: NON-METALLIC ELEMENTS; COMPOUNDS THEREOF; {METALLOIDS OR COMPOUNDS THEREOF NOT COVERED BY SUBCLASS C01C}
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

The present invention provides a novel method for the preparation of 18F-fluoride (18F) for use in radiofluorination reactions. The method of the invention finds use especially in the preparation of 18F-labelled positron emission tomography (PET) tracers. The method of the invention is particularly advantageous where bulk solutions are prepared and stored in prefilled vials rather than being freshly prepared on the day of synthesis. Also provided by the present invention is a radiofluorination reaction which comprises the method of the invention, as well as a cassette for use in carrying out the method of the invention and/or the radiofluorination method of the invention on an automated radiosynthesis apparatus.

## Claims

### Claim at position 1

1-19. (canceled)

### Claim 20

A cassette for carrying out the radiofluorination reaction comprising:
(i) an anion exchange column suitable for trapping an aqueous solution of 18F;
(ii) a first vial containing an eluent solution, wherein the eluent solution comprises a mixture of potassium carbonate and kryptofix in an aqueous alkanol solvent and being devoid of acetonitrile; and
(iii) a second vial containing a precursor compound which upon reaction with 18F— results in an 18F-labelled PET tracer;
wherein said eluent solution is capable of being (i) prepared in bulk and (ii) stored in the first vial prior to use, thereby affording a consistent percentage radiochemical yield of the 18F-labelled PET tracer.

### Claim 21 (depends on 20)

The cassette as defined in claim 20 which further comprises one or more of:
(iv) drying means;
(v) an ion exchange cartridge for removal of excess 18F—;
(vi) a cartridge for removing any protecting groups; and,
(vii) one or more solid-phase extraction cartridges to obtain said 18F-labelled PET tracer in a purified form.

### Claim 22 (depends on 20)

The cassette as defined in claim 20 wherein said anion exchange column is an anion exchange column.

### Claim 23 (depends on 20)

The cassette as defined in claim 20 wherein said anion exchange column is a quaternary methylammonium (QMA) column.

### Claim 24 (depends on 20)

The cassette as defined in claim 20 which is automated.

### Claim 25 (depends on 20)

The cassette as defined in claim 20, wherein the cassette is suitable for use with an automated radiosynthesis apparatus.

### Claim 26 (depends on 20)

The cassette as defined in claim 20, wherein said 18F-labelled PET tracer is 2-deoxy-2-[18F]fluoro-D-glucose, [18F] fluorothymidine, [18F] fluoronitroimidazole, 6-[18F]fluoroDOPA, [18F]setoperone, [18F]altanserin, [18F]N-methylspiperone, 6-[18F] fluorodopamine, (−)6-[18F]fluoro-norepinephrine, I6α-[18F]fluoroestradiol, [18F]fleroxacin or [18F]fluconazole.

### Claim 27 (depends on 25)

The cassette as defined in claim 25, wherein said 18F-labelled PET tracer 1s 2-deoxy-2-[18F]fluoro-D-glucose, [18F]fluorothymidine or [18F]fluoronitroimidazole.

### Claim 28 (depends on 25)

The cassette as defined in claim 25, wherein the 18F -labelled PET tracer is [18F]FDG or [18F]FACBC.