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The synthesis of novel structures related to naturally occurring cardiotonic agents such as resibufogenin is described. These products retain the essential features of aglycones needed for biological activity. They are, however, thermodynamically stable and easily available from smilagenin. The methods of preparation, together with the proof of structures and configuration, are reported.

A series of 7alpha,8alpha-expoxyestradiol derivatives with ethynyl, 2- or 3-furyl, or 2-thienyl substituents in the 17alpha position was prepared. The products were highly active orally in the Allen-Doisy test in rats, but most of them were only weakly active in the uterotrophic assay in the mouse. A 7alpha,8alpha-methylene analog and a 7alpha,8alpha-difluormethylene analog were less active than the corresponding epoxides.