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US 2010/0143252 A1Published application
Imaging 18f or 11c-labelled alkylthiophenyl guanidines
AssigneeHammersmith Imanet Limited
InventorsEdward George Robins, Erik Arstad
Life of this patent
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Abstract
The invention provides a compound of formula (I); or a salt or solvate thereof, wherein: R1 is hydrogen or C1-4alkyl; R2 and R4 are each independently selected from C1-4 alkyl, [11C] C1-4alkyl, and [18F]—C1-4 fluoroalkyl provided that at least one of R2 and R4 is [11C] C1-4alkyl or [18F]—C1-4 fluoroalkyl; and R3 is halo. Such compounds having use for imaging central nervous system receptors.
Claims11
A compound of formula (I):
- or a salt or solvate thereof, wherein:
- R1 is hydrogen or C1-4alkyl;
- R2 and R4 are each independently selected from C1-4 alkyl, [11C]—C1-4alkyl, and [18F]—C1-4 fluoroalkyl provided that at least one of R2 and R4 is [11C]—C1-4alkyl or [18F]—C1-4 fluoroalkyl;
- and
- R3 is halo.
2 more elements
A compound of formula (II):
- or a salt thereof, wherein one of R2 or R4 is hydrogen or a thiol protecting group such as benzyl, and the other is hydrogen, C1-4 alkyl, or a thiol protecting group such as benzyl;
- R1 is hydrogen or C1-4alkyl, and R3 is halo.
A process for preparation of a compound of formula (I):
- or a salt or solvate thereof, wherein:
- R1 is hydrogen or C1-4alkyl;
- R2 and R4 are each independently selected from C1-4 alkyl, [11C]—C1-4alkyl, and [18F]—C1-4 fluoroalkyl provided that at least one of R2 and R4 is [11C]—C1-4alkyl or [18F]—C1-4 fluoroalkyl;
- and
- R3 is halo;
- which comprises reaction of a compound of formula (II):
- wherein one of R2 or R4 is hydrogen or a thiol protecting group such as benzyl, and the other is hydrogen, C1-4 alkyl, or a thiol protecting group such as benzyl;
- R1 is hydrogen or C1-4alkyl, and R3 is halo;
- by (i) removal of any thiol protecting groups, and (ii) reaction with the appropriate alkylhalide [11C]C1-4alkyl-X or [18F]—1-4-fluoroalkyl-Y, wherein X and Y are independently halo, preferably chloro, iodo, or bromo, or another suitable leaving group such as an aryl or alkyl sulphonate, for example, tosylate, triflate, or mesylate;
- in a suitable solvent and in the presence of a base.
7 more elements
Dependencies are inferred from the claim text.