RESUMEN
Condensation between ethyl formate and estradiol 16-keto derivatives, in which the 17beta-hydroxyl groups had been protected as tetrahydropyranyl ethers, produced the corresponding 15-hydroxymethylene compounds. These, by cyclization with hydrazine, gave the [16,15-c]-pyrazole derivatives. Further reactions, such as hydrolysis, etherification and chromic oxidation, afforded many differently substituted [16,15-c]-pyrazoles of the estradiol and estrone series.
Asunto(s)
Estradiol , Estrona , Pirazoles/síntesis química , Esteroides Heterocíclicos/síntesis química , Química FarmacéuticaRESUMEN
The structure-activity relationship of some topically applied 21-desoxy-substituted steroids as anti-inflammatory agents was investigated; the anti-inflammatory activity remained unaltered or increased on introducing a methyl group in position 6alpha and a hydroxyl group in position 11beta, even after eliminating the hydroxyl group in position 21. The activity of the molecule was further increased by the introduction of a hydroxyl group in position 17alpha and a fluorine atom in position 9alpha.