| 摘要 |
1529249 21,22-Disubstituted pregnane compounds SYNTEX (USA) Inc 6 July 1976 [7 July 1975] 28129/76 Heading C2U Novel steroids of the formulae (A), (B), (C) wherein in (A) R<SP>11</SP> is Cl or OH; R<SP>21</SP> is C 1-8 alkyl; X<SP>1</SP> and X<SP>2</SP> are each H, Cl or F, but when R<SP>11</SP> is Cl then X<SP>2</SP> is Cl; Y is OR<SP>21</SP>, SR<SP>21</SP>', Br, Cl, CN, SCN or N 3 in which R<SP>21</SP> is as defined above but independent thereof and R<SP>21</SP>' is C 1-8 alkyl or phenyl; Z is a single or double bond; and in (B) and (C) R<SP>11</SP>, Z and X<SP>2</SP> are as defined above; all R<SP>21</SP>'s are the same C 1-8 alkyl; and X<SP>1</SP>' is H, Cl or F when Z is a single bond and is Cl or F when Z is a double bond, are prepared by the following reaction sequence: wherein R<SP>11</SP>, R<SP>21</SP>, X<SP>1</SP>, X<SP>2</SP>, X<SP>1</SP>' and Z are as defined above; Y is OR<SP>21</SP>, SR<SP>21</SP>', CN, SCN or N 3 in which R<SP>21</SP> and R<SP>21</SP>' are as defined above; and X is Cl or Br. The reagents used in the conversion of (5) to (6) or alkali metal alkoxides, azides, thiocyanates, cyanides and thioalkoxides and thiophenates. Examples illustrate the depicted processes. The novel steroids are anti-inflammatory agents, and they may be made up into pharmaceutical compositions with suitable carriers. |
