| 摘要 |
<p>1,242,981. Steroid 17α,21 - orthocarbonates. FARBWERKE HOECHST A.G. 20 Jan., 1969 [18 Jan., 1968], No. 3081/69. Heading C2U. The inventor comprises compounds of formula in which additional double bonds or epoxy groups are optionally present in the 1,2- and/or 6,7- and/or 9,11- or 11,12-positions, and wherein X is H 2 , (H, or -OH), (H, #-OH), (H, #-Cl), (H, #-F) or oxo, or, when there is present a 9,11- or 11,12-double bond or epoxy group, X is H; Y is H or halo, or, when there is present a 9,11-double bond or epoxy group, Y is absent; Z is H, F, Cl, Br, Me, Et, CN, CHO or CH 2 OH, which atom or group has theα- or #-configuration in the absence of a 6,7-double bond or epoxy groups or has the #-configuration in the presence of a 6,7-epoxy group; R 1 is C 1-10 aliphatic hydrocarbyl; and R 2 is H, =CH 2 , =CHF, =CF 2 , or, in theα- or #-configuration, Me, Et, OH, C 1-3 alkoxy, F, Cl or Br. These compounds are prepared from the corresponding 17α,21-dihydroxy-20-oxo-steroids by reaction with compounds of formula C(OR 1 ) 4 in the presence of an acid catalyst. A 1,2- or 6,7-double bond may subsequently be introduced into products saturated in one or both of these positions. The inventive compounds are stated to possess antiinflammatory, diuretic and gestagenic activities and may be made up with carriers into pharmaceutical compositions for topical and parenteral administration.</p> |
