摘要 |
<p>Prepn. of 17 alpha-hydroxy pregn.- 3-en-3,20-dione 17-ester of formula (I) comprises esterifying corresp. 11-R8-17 alpha-hydroxy cpd. (II). X is H, F or Cl; R1 is H, F, Cl or Me; R2 is H + Halogen, H + OH or O; R3 is H, alpha-Me or beta-me; R4 is 1-16C alkoxoyl, 3-16C cycloalkanoyl, 7-8C aralkanoyl or Ph CO; either Y is H and Y1 is OH, OR4, halo or H, or Y and Y1 are both halo; and R8 is oxo, H + halo or H + trihaloacetoxy. Specifically claimed cpds. include 9 alpha- fluoro- 11- beta, 17 alpha- dihydloxy- 16-beta methyl pregna-1,4-diene- 3, 20 dione 17-heptanoate. (I) are obtd. by a new and efficient route they include known antiinflammatory agents. For topical application, ointments suitably contain 0.01-0.25 wt.% (I). Used e.g. for treating eczema.</p> |