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Abstract

6-O-(3-Methoxycarbonylpropyl)- and 6-O-(3-carboxypropyl)oximes of 16 alpha,17 alpha-cyclohexanopregn-4-ene-3,6,20-trione labeled by tritium in position 1,2 were synthesized. When using homogenous catalysts, the molar radioactivity of the resulting preparations was 1.5-1.7 PBq/mol.

Solid‐phase reactions as approach to the synthesis of organic compounds labelled with tritium

“…14,19 However, for high-melting sodium salts of acetic, propionic and butyric acids, the molar radioactivity did not show this type of unambiguous dependence on the number of carbon atoms (Figure 7). 20 Introduction of a tritium label into compounds of lipid nature by solid-phase isotope exchange…”

“…The chemical yield of hexadecane and cetyl alcohol after the exchange is 80%, whereas labelled compounds containing free amines, neuraminic acid and so on are formed in less than 20% yields. 20,27,32 The stabilities of the specimens can be sharply different even in the case of compounds with similar structures (Table 9). For example, the yield of the sodium salt of N-acetylneuraminic acid a-methyl glycoside at 2008C is almost twice as high as that of the derivative of the trisaccharide sialyllactose at 1608C.…”

Pregna-D′-pentaranes, progestins and antiprogestins: I. Separation of biological functions of steroid hormones

“…We developed the methods of selective hydrogenation of the double bonds either present in the molecule or specially introduced at the final steps of synthesis. The tritium-labeled analogues of pentaranes (Va) and (IV) were obtained by the catalytic homogeneous or heterogeneous hydrogenation with gaseous tritium of their D'-ring-unsaturated precursors (XIVa) [20] and (XVII) [27], respectively. The labeled derivatives (XXIV), (XLIV), and (XLVII) were obtained from the corresponding 1,2-dehydroprecursors (XXV) and (XXVI) using the subsequent separation of the resulting tritiated pentaranes by HPLC [28,29].…”

“…These regularities could only be revealed after a deep insight into the mechanism of the hormonal action of progestins in order to establish the homogeneity of the population of the plasmatic (nuclear) progesterone receptor that mediates the transfer of hormonal signal, the uniformity or branching of this signal, and the dependence of the expression of the corresponding gene on the structure of steroid ligand. This study became possible after the preparation of a set of 3 H-labeled compounds with the separated biological functions, which can play the role of a convenient instrument for studying the mechanisms of accomplishment of these functions [20,[27][28][29].…”

Steroids: reactions and partial synthesis

“…62 The synthesis of tritium labelled 6-oximes of 16α,17αcyclohexanopregn-4-ene-3,6,20-trione has been reported. 63 In studies to combat the development of multiple drug resistance in various cancers, some C-7 analogues of progesterone, e.g. 30, have been found 64 to be potent inhibitors of the P-glycoprotein efflux pump.…”