| abstract |
Haloaryl compounds bearing a defined group or precursor are metalated with either Sn(n-Bu)3 or SnMe 3 . The resulting aryltin compound may be transmetalated in site-specific reaction with one of the following organometallic groups: HgX 2 , Hg(OAc) 2 , BX 3 , or BZ 3 , wherein X is Cl, Br, or I, and Z is alkyl or alkoxy. The stannylated or otherwise metalated compounds are subsequently radiohalogenated via a demetalation reaction. The functional group is suitable for conjugaton to protein and can be present or be added subsequent, but most preferably prior, to the radiohalogenation. n Also compounds of the formula: Ri-Ar-R 2 , wherein R 1 is either a radiohalogen or any one of the organometallic groups stated above, Ar is aromatic or heteroaromatic ring, and R 2 is a short-chain substituent that does not highly activate the aromatic ring and that bears a functional group suitable for conjugation to protein under conditions that preserve the biological activity of the protein. The radiohalogenated small molecules are conjugated to proteins such as monoclonal antibodies for use in diagnosis and therapy. |