Title:
エストロンおよびエストラジオールの2-置換誘導体の調製方法
Document Type and Number:
Japanese Patent JP5075626
Kind Code:
B2
Abstract:
The invention provides a process for the preparation of 2-substituted-derivatives of estrone and estradiol comprising i) the preparation of a compound of general formula (II) by reacting a compound of general formula (I) in one or more steps to a compound of general formula II wherein R1 is a C1-C10 alkyl, alkenyl or aryl group; —Cl, —Br, —I, —F; —CN; —OH; or a —OR2, —O(CO)R2 or —R2-OH group, wherein R2 is an alkyl or alkylene group having 1-6 C atoms; and the bonding between atoms 9 and 10 is a single or a double bond. ii) aromatization of the compound of general formula II to a compound of general formula III wherein R1 and R2 have the above defined meanings; and iii) optionally, reduction of the compound of general formula III to a compound of general formula IV wherein R1 and R2 have the above defined meanings. Furthermore the invention provides several novel compounds, which can be intermediates in the above process, and processes to prepare these novel compounds. The invention also provides 2-alkoxy-estrone, 2-alkoxy-estradiol or mixtures thereof essentially free from other estrogenic intermediates.
Inventors:
Stouhl Binder, Johannes
Moers, Nicolas Elizabeth Cornelis
Moers, Nicolas Elizabeth Cornelis
Application Number:
JP2007524335A
Publication Date:
November 21, 2012
Filing Date:
August 01, 2005
Export Citation:
Assignee:
STICHTING TOP INSTITUTE PHARMA
International Classes:
C07J1/00; A61K31/565; A61K31/566; A61P9/00; A61P9/10; A61P15/08; A61P17/02; A61P19/02; A61P29/00; A61P35/00; A61P37/00; A61P43/00; C07C49/753; C07D311/94; C07D319/06; C07J75/00
Domestic Patent References:
| JP5506438A | ||||
| JP2003507489A | ||||
| JP9183792A |
Foreign References:
| FR1468608B1 | ||||
| US2997488 | ||||
| US4400524 | ||||
| DE3208432A1 | ||||
| US3186907 |
Other References:
BRODIE, H. J.,Studies on the mechanism of estrogen biosynthesis. VII. 2β-Hydroxylation of estr-4-ene-3,17-dione in human placenta, in vitro,Biochimica et Biophysica Acta, Lipids and Lipid Metabolism,1969年,187(2),p. 275-277
Attorney, Agent or Firm:
Kawaguchi International Patent Office
Yoshio Kawaguchi
Makoto Ono
Chihiro Watanabe
Kenkyo Kanayama
Katsuma Osaki
Mitsuaki Tsubokura
Yoshio Kawaguchi
Makoto Ono
Chihiro Watanabe
Kenkyo Kanayama
Katsuma Osaki
Mitsuaki Tsubokura