Reactions of organometallic compounds with astatine-211. Application to protein labeling

The reactions of astatine-211 with six different organometallic compounds have been studied. Initial experiments were carried out with methyl benzoate and toluene compounds containing tri-n-butylstannyl, boronic acid, mercuric chloride, and pentafluorosilicate funcitonalities. The astatine-211 labeling of these compounds resulted in radiochemical yields of 55-80%. Preliminary studies with readily available I-125 defined the reaction conditions for beginning the At-211 studies. All radiolabeling experiments were monitored by radioHPLC to separate the reaction products and determine the radiochemical yields. Other experiments involved the astatination of a protein reactive arylstannane which was labeled and subsequently conjugated to a F(ab')2 fragment of an antibody in 37-55% radiochemical yield. (orig.)