Polymer precursors of radiolabeled compounds, and methods of...

C - Chemistry – Metallurgy – 08 – F

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C08F 8/42 (2006.01) C08F 212/14 (2006.01) C07B 59/00 (2006.01)

Patent

CA 2439448

One aspect of the present invention relates to polymyer precusors Poly-L-R-Y where Poly=poly, L = -Sn(R3)2- or -SN(R3)2-Sn(R3)2-, R= aryl or heteroaryl, Y = hydrogen, alkyl, alkoxyl, carbonyl, formyl, amido, amino, alkylamino, dialkylamino, carboxamido, acylamino, (heterocyclyl)acylamino, alkylcarboxyamido, CO-4 or CO-NH-R4, R3 = alkyl, alkenyl or alkynyl, R4 = hydrogen, alkyl, alkenyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, heteroalkyl, peptide, protein, amino acid, antibody, nucleotide, nucleoside, or (CH2)m-R80 = aryl, cycloalkenyl, heterocyclyl or polycyclyl, and m= 0-8. A second aspect is directed to a method for preparing a radiolabelled compound by reacting said polymer percursor compound with an oxidant, a radiolabelled compound and optionally a buffer. A further aspect is a kit containing a radiolabelling system comprising said polymer precursor compound.and instructions for using said polymer precursor compound. The final aspect is a method for synthesising radiolabelled benzamides on a solid support by (a) selecting as solid support comprising at least one compound comprising a benzoic acid moiety attached to the solid subpport, (b) reacting said moiety of the compound attached to the solid support with at least one amine to afford a benzamide bound to a solid support, and (c) reacting said benzamide bound to said solid support with a radiolabelled compound or isotope and an oxidant to yield said radiolabelled benzamides.

Un premier mode de réalisation de l'invention concerne de nouveaux composés pouvant être utilisés dans la préparation efficace de composés radiomarqués. Un autre mode de réalisation concerne une méthode de synthèse de composés radiomarqués.

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