Radiolabelling reagents and methods
View Patent ↗The present invention relates to reagents and methods for [ 18 F]-fluorination of biomolecules, particularly of peptides. The resultant 18 F-labelled compounds are useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET).
1. A compound of formula (I):
2. A compound according to claim 1 of formula (Ia):
3. A method for 18 F-fluorination comprising reaction of a compound of formula (I) or (Ia) as defined in claim 1 with a compound of formula (III):
to give an 18 F-product of formula (IV) :
4. A method according to claim 3 wherein the biomolecule is a peptide.
5. A method according to claim 3 wherein the biomolecule is a peptide selected from somatostatin analogues, such as octreotide, bombesin, vasoactive intestinal peptide, chemotactic peptide analogues, a-melanocyte stimulating hormone, neurotensin, Arg-Gly-Asp peptide and its analogues, human pro-insulin connecting peptide, endothelin, angiotensin and formyl-norleucyl-leucyl-phenylalanyl-norleucyl-tyrosyl-lysine.
6. A method according to 3 wherein the biomolecule comprises the fragment:
7. A method according to claim 3 wherein the biomolecule is a peptide of formula (A):
wherein X 7 is either —NH 2 or
wherein a is an integer of from 1 to 10.
8. A method according to claim 7 wherein a is 1.