| 摘要 |
Disclosed is a process for producing the epoxy steroid (1.0) wherein R1 is selected from H, -OH, or C1, and R2 is selected from hydrogen or lower alkyl. The process comprises reacting the triene of Formula (2.0) with a brominating or chlorinating agent in DMF containing a catalytic amount of 70 percent HC1O4, at a temperature of about 0 to about +40 degree C to produce the corresponding bromoformate (3.0) or chloroformate (3.0A) wherein when R1 is H then R3 is H; and when R1 is -OH then R3 is a suitably protected -OH group; and when R1 is C1 then R3 is C1. The bromoformate or chloroformate is then reacted, at a temperature of about -20 to about +10 degree C, with a strong base in an organic solvent mixture comprising: (a) THF or CH2C12 and (b) a C1 to C6 alkanol or acetonitrile, to produce the epoxy steroid (1.0).
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