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US 2019/0161440 A1Published application
Alkylation method
AssigneesGe Healthcare Limited, King's College London
InventorsImtiaz KHAN, Graeme MCROBBIE, Anna KIRJAVAINEN
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Abstract
The present invention relates to a method of radiochemical synthesis. Novel methods useful in the synthesis of a positron emission tomography (PET) tracer, and novel intermediates useful in said method are provided that have advantages over known methods.
Claims36
A method to obtain a compound of Formula I:
- wherein:
- (i) X1 is an X group selected from C1-4 alkyl or halo;
- Y1 is a Y group selected from hydrogen or C1-4 alkyl;
- Z1 is a Z group which is C1-4 alkyl;
- and,
- Q is [11C]C1-4 alkyl- or [18F]-C1-4fluoroalkyl-;
- wherein said method comprises:
- (ii) reducing a compound of Formula II:
- wherein:
- (ii) X11 and X12 are the same and are both an X group as defined for X1;
- Y11 and Y12 are the same and are both a Y group as defined for Y1;
- and,
- Z11 and Z12 are the same and are both a Z group as defined for Z1;
- and,
- (ii) adding a base to the product of step (i) and reacting with either [11C]C1-4 alkyl-LG1 or [18F]-C1-4 fluoroalkyl-LG2, wherein LG1 and LG2 are independently halo, or the group —O—SO2—R1 wherein R1 represents an optionally-substituted C6-10 aryl, an optionally-substituted C1-4 alkyl, or C1-4 fluoroalkyl;
- wherein the molar ratio of added base:thiol in step (ii) is in the range of about 0.2-1.0.
13 more elements
The method as defined in claim 32 wherein said SPE is carried out using one or more environmental tC18 SPE cartridges.
Dependencies are inferred from the claim text.