A. Burgos et Gj. Ellames, CONVENIENT SYNTHESIS OF [2-C-14]-METHYLGLYOXAL BIS(GUANYLHYDRAZONE), [C-14] MITOGUAZONE, Journal of labelled compounds & radiopharmaceuticals, 36(1), 1995, pp. 93-96
[2-C-14]-Methylglyoxal bis(guanylhydrazone) dihydrochloride, [C-14]-mi
toguazone, 3, has been prepared in three steps from potassium [1-C-14]
-acetate in an overall radiochemical yield of 16%. The key steps in th
is procedure are the formation of the sodium Salt of [acetone-2-C-14]-
methylsulfinylacetone, 5, and Pummerer rearrangement to the [C-14] lab
elled hemithioacetal, 6, which is trapped with two equivalents of amin
oguanidine to afford the desired [C-14]-mitoguazone, 3.