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    • 4. 发明授权
    • Retrosteroid a-ring formation
    • 回波环形成
    • US3591607A
    • 1971-07-06
    • US3591607D
    • 1966-04-19
    • HOFFMANN LA ROCHE
    • BASEL ANDOR FURSTKOCH WOLFGANGUSKOKOVIC MILAN RADOJE
    • C07C59/205C07C59/215C07C171/07C07D3/00
    • C07C59/205C07C59/215C07C2603/16
    • IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL, HYDROXY, LOWER ALKANOYLOXY; AND HALO; Q, WHEN TAKEN ALONE, IS OXO; T1, WHEN TAKEN ALONE, IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF ALKALI METAL OXY AND LOWER ALKOXY; AND T1 AND Q, WHEN TAKEN TOGETHER, ARE NITRILE. THESE COMPOUNDS ARE INTERMEDIATES WHICH CAN BE CONVERTED TO A KNOWN CLASS OF ENDOCRINOLOGICALLY ACTIVE 9,10-STEROIDS.

      Y-CH2-CO-

      Y IS A MEMBER SELECTED FORM THE GROUP CONSISTING OF HYDROGEN, HALO, AND HYDROXY; R17A, WHEN R17B IS HYDROXY AND LOWER ALKANOYLOXY, IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LOWER ALIPHATIC HYDRCARBYL, AND, WHEN R17B IS

      Y-CH2-CO-

      R17B IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROXY, LOWER ALKANOYLOZY, AND

      >C(-R17B)-R17A

      R1 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKOXY, AND LOWER ALKYLTHIO: R2 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKOXY, AND LOWER ALKYLTHIO; R6 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKYLTHIO, LOWER ALKANOYLTHIO, AND HALO; R7 IS A MEMBER SELECTED FROMTHE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKYLTHIO, LOWER ALKANOYLTHIO, AND HALO; R11 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDORGEN, HYDROXT, AND LOWER ALKANOYLOXY; R16 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, HYDORXY, LOWER ALKOZY, LOWER ALKANOYLOXY, AND, WHEN THE 17B-SUBSTITUENT IS ACETYL OR SUBSTITUTED ACETYL, FLUORINE; Z IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF CARBONYL, (17B-HYDROXY-17A-LOWER ALKANOIC ACID LACTONE), AND

      8-(Q=C(-T1-CH(-R2)-CH(-R1)-)DECALIN

      1-R11,3-C,3,4-(-Z-CH(-R16)-CH2-),5-R7,6-R6,7-(O=),8-CH3,

      3,5-SECO-9B,10A STEROIDS OF THE FORMULA:

      WHEREIN: