发明授权
US06169178A Process for the preparation of 16,17 acetals of pregnane derivatives with control of the epimeric distribution at the C-22 position 失效
制备16,17缩醛的孕烷衍生物的方法,控制C-22位置的差向异构体分布

  • 专利标题: Process for the preparation of 16,17 acetals of pregnane derivatives with control of the epimeric distribution at the C-22 position
  • 专利标题(中): 制备16,17缩醛的孕烷衍生物的方法,控制C-22位置的差向异构体分布
  • 申请号: US09067711
    申请日: 1998-04-28
  • 公开(公告)号: US06169178A
    公开(公告)日: 2001-01-02
  • 发明人: Filippo La LoggiaPaolo Petacchi
  • 申请人: Filippo La LoggiaPaolo Petacchi
  • 优先权: ITMI97A0111 19970430
  • 主分类号: C07J7100
  • IPC分类号: C07J7100
Process for the preparation of 16,17 acetals of pregnane derivatives with control of the epimeric distribution at the C-22 position
摘要:
Described herein is a process for the preparation of an acetal of formula (I) in which R1 is an alkyl, R2 is H or an acyl, X is &bgr;-OH and Y is H, comprising the acetalization with control of the epimeric distribution at the C-22 position, for treatment with R1 CHO in aqueous HBr or HI of a compound of formula (II) in which R2 has the meaning specified above, R3 and R4 are both H, or, taken together, are —C(R5)(R6)—, where R5 and R6, which may be the same or different from one another, are alkyl groups, and X and Y are chosen from among the following: A) X and Y, taken together, are an additional bond between C-9 and C-11; B) X is &bgr;-OH, and Y is H or an &agr;-halogen; C) X is &bgr;-OR7 where R7 is an acyl, and Y is H or an &agr;-halogen; and D) X and Y, taken together, are —O—.
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