POLYMER PRECURSORS OF RADIOLABELED COMPOUNDS, AND METHODS OF MAKING AND USING THE SAME

摘要

One aspect of the present invention relates to polymyer precursors 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 heterocyclyl, 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 precursor compound with an oxidant, a radiolabelled compound, and optionally a buffer. A further aspect is a kit containing a radilabelling system comprising said polymer precursor compound and instructions for using said polymer precursor compound. The final aspect is a method for synthesizing radilabelled benzamides on a solid support by a (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 radilabelled compound or isotope and an oxidant to yield said radilabelled benzamides.