EFFICIENT SYNTHESIS OF CHELATORS FOR NUCLEAR IMAGING AND RADIOTHERAPY: COMPOSITIONS AND USE Russian patent published in 2014 - IPC C07C323/57 A61K47/48 A61K49/00 A61K51/04 A61P9/00 A61P35/00 C07H5/00 C07C323/58 

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 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 R₁, R₂, R₃ and R₄ is H; X denotes -CH₂-CH₂-; 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 ^99mTc- ethylenedicysteine (EC)-glucosamine, ¹⁸⁸Re-EC-glucosamine or ¹⁸⁷Re-EC-glucosamine.

EFFECT: method enables to products of high purity.

10 cl, 13 dwg, 4 tbl, 18 ex