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Title:
7―アルファ―カルボキシル―9,11―エポキシステロイド化合物の製造方法およびこの方法に有用な中間体ならびにオレフィン二重結合の一般的エポキシ化方法
Document Type and Number:
Japanese Patent JP4146897
Kind Code:
B2
Abstract:
Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I wherein: -A-A- represents the group -CHR4-CHR5- or CR4-CR5- R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy, R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical, -B-B- represents the group -CHR6-CHR7- or an alpha- or beta-oriented group: where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, and R8 and R9 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or R7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring.

Inventors:
Ng, John, S.
Wang, Ping, Tee.
Baez, Julio, A.
Riu, Shin
Anderson, Dennis, Kay.
Lawson, Yong, Pee.
Elves, Dane Hard
Wiekzorek, Joseph
Musialier, Genaro
Banzanera, Fortunet
Kunda, Sustain, A.
Retendre, Leo, Jay.
Pozo, Mark, Jay.
Sing, Yuen-Lung, El.
Application Number:
JP52230497A
Publication Date:
September 10, 2008
Filing Date:
December 11, 1996
Export Citation:
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Assignee:
G.D.Searle & Company
International Classes:
C07J71/00; A61K31/58; C07J1/00; C07J9/00; C07J19/00; C07J21/00; C07J31/00; C07J53/00; C07J75/00; C12P33/00; C12P33/10; C12Q1/02
Domestic Patent References:
JP5053363A
Foreign References:
US3200113
Other References:
BROWN, E. A., ET AL, JOURNAL OF MEDICINAL CHEMISTRY, 1963年, vol.6, no. 6, pages 732-735
BROWN, E.A., ET AL, JOURNAL OF ORGANIC CHEMISTRY, 1960年, vol. 25, no. 1, pages 96-99
CHRISTIANSEN, R., ET AL, STEROIDS, 1960年, vol. 1, no. 6, pages 620-627
WEIER, R. M., ET AL, JOURNAL OF MEDICINAL CHEMISTRY, 1975年, vol.18, no. 8, pages 817-821
Attorney, Agent or Firm:
Hideto Asamura
Hajime Asamura
Naganuma Akio
Yukihiro Ikeda