STEROID WITH 17-SPIROMETHYLENELACTONE GROUP AND METHOD OF ITS SYNTHESIS Russian patent published in 2001 - IPC

FIELD: organic chemistry, steroids. SUBSTANCE: invention relates to novel steroids, namely to steroid with 17-spiromethylenelactone group of the general formula (I) where R₁ is O, (H,H), (H,OR) or NOR being R is taken among H, (1-6C)-alkyl and (1-6C)-acyl; R₂ is H, (1-6C)-alkyl that can be substituted arbitrarily with halogen atom, (2-6C)-alkenyl that can be substituted with halogen atom arbitrarily, (2-6C)-alkynyl that can be substituted with hydrogen or halogen atom arbitrarily; R_2′ is H; or R_2′ in common with c₂ is (1-6C)-alkylidene group or (2-6C)-alkenylidene group; or R_2′ in common with R₃ present the bond; R₃ is H if in common with R_2′ is not the bond; R₄ is (1-6C)-alkyl; one of R₅ and R₆ is hydrogen atom and other one is hydrogen atom or (1-6C)-alkyl; X means (CH₂)_n or (C_nH_2n-2) where n = 2 or 3 which is substituted arbitrarily with hydroxyl, halogen atom, (1-6C)-alkyl, (1-6C)-acyl, (7-9C)-phenylalkyl being the latter phenyl group can be substituted with (1-6C)-alkyl, (1-6C)-alkoxyl, hydroxyl or halogen atom; Y is O or (H, OH) and dotted lines show arbitrary bonds being at least one of bonds 4-5, 5-10 and 9-10 is the double bond. Invention describes method of synthesis of compounds of the formula (I). Synthesized compounds elicite significant antiglucocorticoidal and antiprogestagenic activity. EFFECT: new steroids indicated above, improved method of synthesis, valuable medicinal activities. 6 cl, 2 tbl, 29 ex