5 beta -Hydroxy- DELTA 6-steroids and process for the preparation thereof

摘要

PCT No. PCT/DE81/00111 Sec. 371 Date Mar. 11, 1982 Sec. 102(e) Date Mar. 11, 1982 PCT Filed Jul. 2, 1981 PCT Pub. No. WO82/00294 PCT Pub. Date Feb. 4, 1982.The disclosure concerns 5 beta -hydroxy- DELTA 6-steroids of the general formula <IMAGE> wherein R1 is hydrogen, acyl, lower alkyl, or the tetrahydropyranyl residue and R2, R3 individually are respectively hydrogen or jointly are methylene and X stands for oxygen, the groupings <IMAGE> <IMAGE> (wherein R4 means hydrogen or acyl) and <IMAGE> (wherein R5 means hydrogen or lower alkyl) and a process for the preparation thereof by reacting corresponding 7 alpha -chloro-5 beta ,6 beta -epoxy steroids in an inert solvent with metallic zinc in a lower aliphatic carboxylic acid or dilute mineral acid at temperatures of between room temperature and 100 DEG C., preferably at 40 DEG -70 DEG C. The compounds producible by this method are intermediates for the preparation of 3-keto- DELTA 4-6 beta ,7 beta -methylene steroids constituting pharmacologically valuable compounds, for example aldosterone antagonists.