abstract |
FIELD: chemistry. n SUBSTANCE: invention relates to a method for synthesis of chelator-targeting ligand conjugates, which can be used to treat and diagnose diseases, e.g., by imaging tumours or myocardial ischaemia. The method includes step (a) for conjugating, in an organic medium, a chelator of formula with at least one unprotected targeting ligand, which is glucosamine, where each of A and D is a protected thiol, each of B and C is a protected secondary amine; each of E and F is a -COOH group; each of R 1 , R 2 , R 3 and R 4 is H; X denotes -CH 2 -CH 2 -; and where conjugation occurs through formation of an amide bond between E or F of the chelator and the amino group of the glucosamine. The organic medium used is usually a polar or nonpolar solvent or a mixture thereof. The method can further include (b) purifying the conjugate of the chelator-targeting ligand; step (c) of chelating a metal ion with the conjugate of the chelator-targeting ligand to form a metal ion-labelled chelator-targeting ligand conjugate. Step (c) includes a step (d) of removing at least one protective group from the metal ion-labelled chelator-targeting ligand conjugate or additionally a step (e) of adding a reducing agent. The preferred conjugates are 99m Tc- ethylenedicysteine (EC)-glucosamine, 188 Re-EC-glucosamine or 187 Re-EC-glucosamine. n EFFECT: method enables to products of high purity. n 10 cl, 13 dwg, 4 tbl, 18 ex |