Vinyl substituted radiohalogen conjugates for protein labeling

摘要

Vinyl radiohalogenated small molecules as shown in formulas I and II: ##STR1## wherein *X is radiohalogen, C═C is a double bonded set of sp. sup.2 hybridized carbon atoms, and substituents R.sub.1, and R. sub.2 are as defined in the specification. Y is a substituent containing any of the groups described for R.sub.1 and R.sub.2, except that Y cannot be hydrogen, and bearing a functional group suitable for binding to protein under conditions that preserve the biological activity of the protein. The compounds of formulas I and II can be coupled to proteins such as monoclonal antibodies to provide reagents for diagnostic and therapeutic applications. Also metalated precursors of compounds I and II, as well as radiopharmaceutical reagent kits containing any of the subject small molecules.