Synthesis and screening of bifunctional radiolabelled carborane-carbohydrate derivatives

A new bifunctional carborane ligand was prepared as a platform for the development of targeted molecular radioimaging and therapy agents. The carborane derivative was synthesized bearing a glucose substituent to increase the water solubility of the ligand and a benzoic acid group as a site for linking to amine containing targeting vectors. A convenient method to conjugate the ligand and the non-glycosylated analogue to amino groups was developed using simple active esters which were combined with a model amine generating two new N,N-diethyl(aminoethyl) benzamide derivatives. These were labelled with ¹²⁵I in good yield and the log P values measured for [¹²⁵I]-15 (log P = 0.82 ± 0.04) and [¹²⁵I]-16 (log P = 1.53 ± 0.01). The benzamides were also evaluated for their capacity to bind to B16F10 melanoma cells where the hydrophilic compound showed low binding while [¹²⁵I]-16 showed modest uptake (30.7 ± 2.2%) after 24 h.     

Validation of a quantitative procedure for the extraction of sterols from edible oils using radiolabelled compounds

The work described in this paper is integrated in an analytical programme organised by the Community Bureau of Reference with the aim of developing reference materials certified for sterol content. Preliminary inter-comparison of methods showed that the level of agreement of the results was insufficient for certification purposes. Errors could occur in the different steps before the final determination by gas-liquid chromatography. It was, therefore, decided to validate a quantitative procedure for the isolation of sterols. A well defined saponification-extraction method was tested using labelled sterols ([3H]cholesterol and [3H]cholesteryl oleate) and radiochemical measurements. The study has shown that total cholesterol recovery reached 100.5 +/- 1.4%, that cholesteryl ester was saponified quantitatively and that there were no appreciable amounts of degradation products. The procedure has been used as the basis for the certification of three reference materials and it has been shown that the saponification and extraction procedure leads to the quantitative recovery of sterols regardless of the nature of the fatty material tested.     

钴萘酞菁的合成

采用Diels-Alder方法合成了2,3-萘二腈和6,7-二溴-2,3-萘二腈化合物,并以此为前体成功地合成了相应的钴萘酞菁系列化合物---一种新型的功能有机材料。另外还探讨了酞菁形成的机理,并讨论了若干影响因素。这些化合物具有较好的稳定性,在胺类或其它含氮的有机溶剂中有较好的溶解度,如苯胺、二甲基甲酰胺(DMF)或吡啶等。     

Synthesis of macrocyclic compounds

New representatives of macrocyclic ansa-ketolactones that include a thiophene ring, the differences in the yields of which during intramolecular acylation under high-dilution conditions were compared with the peculiarities of their three-dimensional structures, were synthesized. The mass spectra of the ketolactones were studied.See [1] for communication XVII.Translated from Khimiya Geterotsiklicheskikh, Soedinenii, No. 1, pp. 40–44, January, 1975.     

缩杂环卓酮化合物的合成

本文报道Friedlaender反应在卓酮化学中的应用, 合成了喹啉基取代的卓酮化合物。     

Synthesis of organomercury nitro compounds

Summary The mechanism of the addition of the mercury salt of trinitromethane to unsaturated compounds was studied.