Abstract
Microwave-assisted solid-phase synthesis of nicotinyl hydrazones for use in radiochemistry of technetium-99m
Highlights
One of the most useful isotopes in nuclear medicine is the metastable 99mTc.[1]
Since conjugation reactions occur with a molar excess of HYNIC and the reagent hydrazino group could be in the free state in aqueous solution, it is likely that the activated ester reacts with the highly nucleophilic hydrazino group, leading to HYNIC polymerization reactions
We have recently developed for the first time to our knowledge, a microwave-assisted organic synthesis methodology to obtain HYNIC derivatives protected with tert-Butyloxycarbonyl group DCC (Boc) and TFA group.[4]
Summary
One of the most useful isotopes in nuclear medicine is the metastable 99mTc.[1]. Technetium chemistry is based on the formation of complexes in which the metal acts as an electron acceptor from atoms or functional groups capable of donating electrons.2 99mTc is obtained from a generator, pertechnetate anion 99mTcO4– (+7), which must be reduced to a lower oxidation state with high chemical reactivity to be incorporated by a chelating agent. When labeling with 99mTc, the deprotection occurred in one step (Scheme 1).[11,12] Here, we present the synthesis of Suc-HYNIC hydrazone and its derivatization through MASS methodology. The route designed to obtain Suc-HYNIC-hydrazone through microwave-assisted solid-phase synthesis is shown in Scheme 2.
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