Title:
モルフィナンおよびモルフィノン化合物の調製法
Document Type and Number:
Japanese Patent JP5824448
Kind Code:
B2
Abstract:
The present application describes processes for the synthesis of morphinane and morphinone compounds, useful as pharmaceutical agents. Also included are novel intermediates useful in the preparation of these compounds. The process comprises quaternization of oripavine to provide a mixture of the R- and S-isomeric (at the nitrogen) quaternary salts. The R-isomer is readily isolated and converted to various N-(R)-morphinane and N-(S)-morphinone compounds. The R-isomer, S-isomer or a mixture of R- and S-isomers may be demethylated and converted to various morphinane and morphinone compounds.
Inventors:
Hadly Key Thomas
Carol robert
Reish Hanes
Machala Ares
Warner Lucas
Adams David Earl.
Carol robert
Reish Hanes
Machala Ares
Warner Lucas
Adams David Earl.
Application Number:
JP2012506298A
Publication Date:
November 25, 2015
Filing Date:
April 22, 2010
Export Citation:
Assignee:
Block university
International Classes:
C07D489/02
Domestic Patent References:
| JP2006500326A | ||||
| JP2008542287A | ||||
| JP10059849A |
Foreign References:
| WO2009003270A1 | ||||
| WO2001013909A1 | ||||
| WO2008070658A1 |
Other References:
MANOHARAN,T. S.,ET AL.,"Stereoselectivity in Quaternization of Thebaine: 270 MHz PMR Spectroscopic Studies",INDIAN JOURNAL OF CHEMISTRY,SECTION B: ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY,1987年,VOL.26B,NO.2,PP.140-142
MANOHARAN,T. S.,ET AL.,"A Convenient Method for Replacing the N-Methyl Group of Morphine, Codeine, and Thebaine by Other Alkyl Groups",SYNTHESIS,1983年,NO.10,PP.809-812
BOGNAR,R.,ET AL.,"Selective Quaternization in the Morphine Series",TETRAHEDRON LETTERS,1964年,NO.39,PP.2867-2871
LOPEZ, D.,ET AL.,"Photooxidation of Thebaine. A Route to 14-Hydroxymorphinones and Hydrodibenzofuran Analogs of Methadone",TETRAHEDRON LETTERS,1994年,VOL.35,NO.31,PP.5727-5730
MANOHARAN,T. S.,ET AL.,"A Convenient Method for Replacing the N-Methyl Group of Morphine, Codeine, and Thebaine by Other Alkyl Groups",SYNTHESIS,1983年,NO.10,PP.809-812
BOGNAR,R.,ET AL.,"Selective Quaternization in the Morphine Series",TETRAHEDRON LETTERS,1964年,NO.39,PP.2867-2871
LOPEZ, D.,ET AL.,"Photooxidation of Thebaine. A Route to 14-Hydroxymorphinones and Hydrodibenzofuran Analogs of Methadone",TETRAHEDRON LETTERS,1994年,VOL.35,NO.31,PP.5727-5730
Attorney, Agent or Firm:
Hatsushi Shimizu
Masao Haruna
Hirotaka Yamaguchi
Toshi Gobe
Ryuichi Inoue
Toshimitsu Sato
Koichi Niimi
Tomohiko Kobayashi
Masato Ozeki
Yoshihiro Igarashi
Kazuya Kawamoto
Masao Haruna
Hirotaka Yamaguchi
Toshi Gobe
Ryuichi Inoue
Toshimitsu Sato
Koichi Niimi
Tomohiko Kobayashi
Masato Ozeki
Yoshihiro Igarashi
Kazuya Kawamoto