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US 7,264,792 B2Granted
Solid phase preparation of 18F-labelled amino acids
AssigneeGe Healthcare Limited
InventorsAlexander Mark Gibson, Lynda Jane Brown, Richard Charles Downie Brown
Life of this patent
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Abstract
A process for the production of an 18F-labelled tracer which comprises treatment of a solid support-bound precursor of formula (I): SOLID SUPPORT-LINKER-SO2—O-TRACER (I) with 18F— to produce the labelled tracer of formula (II)
Claims13
A process for the production of an 18F-labelled tracer which comprises treatment of a solid support-bound precursor of formula (I):
- SOLID SUPPORT-LINKER-SO2—O-TRACER (I)
- wherein the TRACER is of formula (A):
- wherein P1 is hydroxy or a protecting group, P2 and P3 are independently hydrogen or a protecting group, R1 is a bond, —CH═CH—, or together with R2 forms R3;
- R2 is hydrogen or together with R1 forms R3;
- such that
- is formed
- wherein x is 0 or 1;
- y is 1 or 2;
- z is 1, 2, 3, or 4 and z>y if y is 2;
- q is 1 or 0 if n is 1 and j is 0;
- n is 1 or 2, but 0 if m is 0;
- m is 0 or 1;
- and
- j is 0 or 1;
- with 18F−to produce the labelled tracer of formula (II)
- wherein R1, R2, y, z, P1, P2 and P3 are as defined for the compound of formula (I), optionally followed by
- (i) removal of excess 18F−, for example by ion-exchange chromatography;
- and/or
- (ii) removal of any protecting groups;
- and/or
- (iii) removal of organic solvent;
- and/or
- (iv) formulation of the resultant compound of formula (II) as an aqueous solution.
20 more elements
A compound of formula (I)
- SOLID SUPPORT-LINKER-SO2—O-TRACER (I)
- wherein the TRACER is of formula (A):
- wherein P1 is hydroxy or a protecting group, P2 and P3 are independently hydrogen or a protecting group, R1 is a bond, —CH═CH—, or together with R2 forms R3;
- R2 is hydrogen or together with R1 forms R3;
- such that
- is formed
- wherein x is 0 or 1;
- y is 1 or 2;
- z is 1, 2, 3, or 4and z>y if y is 2;
- q is 1 or 0 if n is 1 and j is 0;
- n is 1 or 2,but 0 if m is 0;
- m is 0 or 1;
- and
- j is 0 or 1.
11 more elements
A compound of formula (Ia):
- wherein P2a and P3a are each independently hydrogen or a protecting group, and P1a is hydroxyl or a protecting group.
Dependencies are inferred from the claim text.