| 摘要 |
1377527 6,7 - Epoxy - 19 - nor - pregnane compounds CIBA-GEIGY AG 2 Feb 1972 [5 Feb 1971] 4849/72 Heading C2U Novel steroids of the formula (wherein R 1 is a free or esterified hydroxyl group) are prepared by treating steroids of the formula (wherein R 1 and R 2 are free or esterified hydroxyl groups and X is a leaving group) with a basic reagent in an inert solvent. In the products a free 17-hydroxy group may be esterified and an esterified 17-hydroxy group hydrolysed. X is suitably a halogen atom or a hydroxy group esterified with an aromatic or aliphatic sulphonic acid or with an aromatic carboxylic acid which carries an activating substituent or substituents in the ortho-and/or para-position. Steroids of the second general formula above wherein X is a halogen are prepared by treating corresponding #<SP>4,6</SP> - 3 - oxo - 19 - norpregnadienes with reagents which add on hypohalous acid. Thus #<SP>4</SP>-3,20-dioxo-6#-hydroxy-7α-chloro- 17α-acetoxy-19-nor-pregnene is prepared by heating #<SP>4,6</SP> - 3,20 - dioxo - 17α - acetoxy - 19 - norpregnadiene with tert.-butyl hypochlorite in formic acid and hydrolysing the resulting #<SP>4</SP>- 3,20 - dioxo - 6# - formyloxy - 7α - chloro - 17α acetoxy-19-nor-pregnene. The novel steroids are gestagens and are suitable for controlling fertility. They may be made up into pharmaceutical compositions with suitable carriers. |
