Abstract

ω-Iodoalkyl(methyl)malonate esters have potential utility in the bioconjugate chemistry of steroids. A representative set of these esters with a variety of protecting groups and alkyl groups has been prepared. The compounds offer a range of elution values on silica, as well as several convenient deprotection options. ω-Bromoalkyl(methyl)malonate esters are precursors of chalcogenobarbiturates, which, in radiolabeled form, may be useful as brain imaging agents.[1] Recently, we have become interested in the analogous ω-iodoalkyl(methyl)malonate esters because of their possible utility in the bioconjugate chemistry of steroids. It is known that steroids can be conjugated to platinum through a malonate moiety.[2] Such platinated steroids are significant because of their potential as tissue-selective antitumor agents.

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