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Title:
ISOMERIZATION OF EQUILIN
Document Type and Number:
Japanese Patent JP3845482
Kind Code:
B2
Abstract:

PROBLEM TO BE SOLVED: To isomerize an equilin into a delta (8,9)-dehydroestrone easily convertible to a component of a composite estrogen composition for hormone exchange therapy, etc., by treating an equilin with ethylenediamine Li salt or Li amide.
SOLUTION: An equilin expressed by formula I [R1 is H, an alkyl, an acyl or a silyl(alkyl)3; R2 is H and R3 is OH, an O-acyl, an O-alkyl or an O-silyl(alkyl)3 or R3 is H and R2 is OH, an O-acyl, an O-alkyl or an O-silyl(alkyl)3 or both of R2 and R3 are O or both of R2 and R3 are acetal or cycloacetal] or its derivative is treated with ethylenediamine lithium salt or lithium amide in dimethyl sulfoxide to isomerize the equilin to delta(8,9)-dehydroestrone of formula II or its derivative.


Inventors:
Petrus Hendrix Raille McAlls
Application Number:
JP28996796A
Publication Date:
November 15, 2006
Filing Date:
October 31, 1996
Export Citation:
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Assignee:
Akzo Novel N B
International Classes:
C07J1/00; A61K31/566; A61K31/57; A61K31/575; A61K31/58; C07J21/00; C07J51/00; C07J75/00; (IPC1-7): C07J1/00; C07J75/00
Foreign References:
US5395831
Other References:
C.R.SEANCES ACAD.SCI.,SER.C,Vol.274, No.10,pp.969-971
Tetrahedrone,1979, Vol.35, No.13,pp.1591-1594
Attorney, Agent or Firm:
Yoshio Kawaguchi
Toru Nakamura
Takeshi Funayama