Abstract: Haloaryl compounds bearing a defined functional group or precursor are metalated with either Sn(n-Bu).sub.3 or SnMe.sub.3. The resulting aryltin compound may be transmetalated in site-specific reaction with one of the following organometallic groups: HgX.sub.2, Hg(OAc).sub.2, BX.sub.3, or BZ.sub.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 Stannylated or otherwise metalated compounds are subsequently radiohalogenated via a demetalation reaction. The functional group is suitable for conjugation to protein and can be present or be added subsequent, but most preferably prior, to the radiohalogenation.Also compounds of the formula: R.sub.1 --Ar--R.sub.2, wherein R.sub.1 is either a radiohalogen or any one of the organometallic groups stated above, Ar is aromatic or heteroaromatic ring, and R.sub.

Abstract: The present invention relates to a novel family of Technetium chelating agents (ligands) based upon amide and mercaptide donor groups.

Abstract: A new series of technetium chelating agents based on amide and mercaptide donor groups is described, exemplified by 2,3-bis(mercaptoacetamido)propanoic acid. Chelation of Tc-99 m with 2,3-bis(mercaptoacetamido)propanoic acid resulted in two components that were separable by high-performance liquid chromatography. The component that eluted first demonstrated high specificity for renal excretion with over 90% in the urine in rabbits at 35 minutes and 87% in the urine of mice at 2 hours and 1.6% or less in the intestines of mice. Excretion was rapid with the first component equal to or greater than I-131 Hippuran in the urine of rabbits at all times. The second or latter component demonstrated comparable specificity, but slower renal excretion kinetics. 2,3-Bis-(mercaptoacetamido)succinic acid forms similar chelates with technetium which are also useful as radiopharmaceuticals for the renal systems of mammals.