The Synthesis of Halogenated Radiopharmaceuticals Using Organomercurials

Abstract

Organomercury chemistry began in 1852 with the synthesis of dimethylmercury by Frankland¹. Since that time thousands of organomercurials have been described. One of the most attractive aspects of organomercury chemistry is the wide range of compounds reported in the literature. Organomercury compounds are known in all the major families of organic compounds, and aliphatic, vinylic, aromatic and heterocyclic compounds have been prepared with relative ease. In contrast with many other organometallic compounds, organomercury compounds have been described in which the mercury group is present in the molecule with other reactive functional groups. Mercury substitution is usually compatible with alcohols, ketones, esters, amides, carboxylic acids, aldehydes and most nitrogen containing groups. Since radiopharmaceuticals are usually molecules with complex substitution patterns, it is this special ability of mercury groups to coexist with other functionalities and yet offer enhanced reactivity for halogenation, that makes them so attractive as intermediates in radiopharmaceutical chemistry.