| 摘要 |
FIELD: chemistry.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 formulawith 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, R, Rand Ris H; X denotes -CH-CH-; 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 areTc- ethylenedicysteine (EC)-glucosamine,Re-EC-glucosamine orRe-EC-glucosamine.EFFECT: method enables to products of high purity.10 cl, 13 dwg, 4 tbl, 18 ex |
