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.
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机译:DELTA3-A-正雄烯基(I或II):( R =低级烷基或芳烷基; R1,R2 = OH或Oacyl; X =卤素,9(11)-饱和或环氧环氧)是抗氧化剂-雄激素,特别是。 11α-羟基-AD或其甲磺酸酯; DELTA3,9(11)-AD; 9alpha-halo-11beta-hydroxy-或acetoxy-AD; 9β,11β-环氧-AD; 9alpha-fluoro-AT,其二乙酸盐和三乙酸盐; (AD = DELTA3-A-nor-androstone-2,17-dione,AT =相应的2beta,11beta,17beta-triol)。准备经由DELTA3,9(11)-AD从11alpha-hydroxy-AD的磺酰基酯中,在二恶烷中用AcNHBr和HClO4处理成9alpha-bromo-11beta-hydroxy-AD(也通过微生物学方法),并通过9beta ,11beta-环氧cpd。,变成9alpha-halo-11beta-羟基类固醇。
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