Patent ID: 8865125

Claim:
A method of radioiodination of a biological targeting moiety, said method comprising: (i) provision of a compound of Formula (Ia) or (Ib): (ii) reaction of said compound of Formula (Ia) or (Ib) with a compound of Formula (II): in the presence of a click cycloaddition catalyst, to give a conjugate of Formula (IIIa) or (IIIb) respectively via click cycloaddition: wherein: I* is a radioisotope of iodine; L 1 comprises a group of formula -(A) m - wherein each A is independently —CR 2 —, —CR═CR—, —C≡C—, —CR 2 CO 2 —, —CO 2 CR 2 —, —NRCO—, —CONR—, —NR(C═O)NR—, —NR(C═S)NR—, —SO 2 NR—, —NRSO 2 —, —CR 2 OCR 2 —, —CR 2 SCR 2 —, —CR 2 NRCR 2 —, a C 4-8 cycloheteroalkylene group, a C 4-8 cycloalkylene group, a C 5-12 arylene group, or a C 3-12 heteroarylene group, an amino acid, a sugar or a monodisperse polyethyleneglycol (PEG) building block; wherein each R is independently chosen from: H, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, C 1-4 alkoxyalkyl or C 1-4 hydroxyalkyl; and m is an integer of value 1 to 20; BTM is the biological targeting moiety chosen from: a single amino acid, a 3-100 mer peptide, an enzyme substrate, an enzyme antagonist, an enzyme agonist, an enzyme inhibitor or a receptor-binding compound.