Title:
【発明の名称】17α-エチニル-17β-ヒドロキシ-18-メチル-4,15-エストラジエン-3-オンの製造方法、及びこの方法の中間生成物
Document Type and Number:
Japanese Patent JP2752366
Kind Code:
B2
Abstract:
1. Process for the manufacture of 17 alpha-ethynyl-17 beta-hydroxy-18-methyl-4,15-estradien- 3-one of the formula I see diagramm : EP0285548,P6,F1 characterised in that a 17-enol ester of the general formula II see diagramm : EP0285548,P6,F2 wherein R1 represents an alkyl radical having 1-3 carbon atoms and R2 represents an acyl or a trialkylsilyl group having up to 10 carbon atoms, is reacted with palladium catalysis to form compounds of the general formula III see diagramm : EP0285548,P6,F3 wherein R1 represents an alkyl radical having 1-3 carbon atoms, and, in a manner known per se, the 17-keto group is reduced, the aromatic A-ring is reacted by the Birch reaction with liquid ammonia to form the corresponding 3-alkoxy-2,5(10),15-estratrien-17 beta-ol, the 17-hydroxy group is reoxidised to the 17-keto group, the 17-keto group is ethynylated and the 3-enol ether is cleaved.
Inventors:
RORUFU BOORUMAN
HENRII RAURENTO
HERUMUUTO HOOFUMAISUTAA
RUUDORUFU UIIHIERUTO
HENRII RAURENTO
HERUMUUTO HOOFUMAISUTAA
RUUDORUFU UIIHIERUTO
Application Number:
JP7350388A
Publication Date:
May 18, 1998
Filing Date:
March 29, 1988
Export Citation:
Assignee:
SHEERINGU AG
International Classes:
C07J1/00; C07J13/00; A61K31/565; C07J75/00; (IPC1-7): C07J1/00
Domestic Patent References:
| JP4615618B1 |
Attorney, Agent or Firm:
Toshio Yano (1 outside)