Synthesis and evaluation of radioiodinated derivatives of 1-azabicyclo[2.2.2]oct-3-yl .alpha.-hydroxy-.alpha.-(4-iodophenyl)-.alpha.-phenylacetate as potential radiopharmaceuticals

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Abstract
Two derivatives of (RS)-1-azabicyclo[2.2.2]oct-3-yl (RS)-.alpha.-hydroxy-.alpha.-(4-iodophenyl)-.alpha.-phenylacetate and 3 partially resolved (R)- or (S)-1-azabicyclo[2.2.2]oct-3-yl (RS)-.alpha.-hydroxy-.alpha.-(4-iodophenyl)-.alpha.-phenylacetates labeled with no carrier added 125I and 123I were synthesized by the Wallach triazene approach. This approach is necessary to obtain no-carrier-added labeling and gives far better results than the direct electrophilic iodination. The obtained yields were 7-18% when using 123I (yield dependent on the source of iodide) and up to 17% for 123I (yield dependent on the source of iodide) and up to 17% for 125I labeled compounds. [(RS)-1-azabicyclo[2.2.2]oct-3-yl-(RS)-.alpha.-hydroxy-.alpha.(4-[125I]iodophenyl)-.alpha.-phenylacetate] localizes in the organs having a large concentration of muscarinic receptors; this localization is due to binding to those receptors in rats.

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