| 摘要 |
<p>DELTA3-A-nor-androstenes (I or II): (R = lower alkyl or aralkyl; R1, R2 = OH or Oacyl; X = halogen, 9(11)-posn. satd. or epoxy gp.), are anti-androgenics, esp. 11alpha-hydroxy-AD or its mesylate; DELTA3, 9(11)-AD; 9alpha-halo-11beta-hydroxy- or acetoxy-AD; 9beta,11beta-epoxy-AD; 9alpha-fluoro-AT, its di- and tri-acetate; (AD = DELTA3-A-nor-androstone-2,17-dione, AT = the corresp. 2beta,11beta,17beta-triol). Prepd. from the sulphonyl-ester of 11alpha-hydroxy-AD via the DELTA3,9(11)-AD, this treated with AcNHBr and HClO4 in dioxan to 9alpha-bromo- 11beta-hydroxy-AD (also obtained microbiologically), and via the 9beta,11beta-epoxy cpd., to the 9alpha-halo-11beta-hydroxysteroid.</p> |
