Title:
ソリフェナシンおよびその塩の製造方法
Document Type and Number:
Japanese Patent JP2014520126
Kind Code:
A
Abstract:
The invention provides a new process for the preparation of solifenacin or a pharmaceutically acceptable acid addition salt thereof, comprising reacting (R)-quinuclidin-3-yl phenethylcarbamate with benzaldehyde in the presence of an acid to obtain a diasteroisomeric mixture (S,R)—((R)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate of formula (IV) which can be resolved and the solifenacin or a pharmaceutically acceptable acid addition salt thereof recovered. The invention also provides the new key intermediate (R)-quinuclidin-3-yl phenethylcarbamate involved in the process. Further the invention provides a method for the transformation of (R)—((R)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate into a diasteroisomeric mixture (S,R)—((R)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate.
Inventors:
ホルディ, ベッサ, Belle Mund
A marina, Corbella, morat
A marina, Corbella, morat
Application Number:
JP2014516204A
Publication Date:
August 21, 2014
Filing Date:
June 22, 2011
Export Citation:
Assignee:
イソケム
International Classes:
C07D453/02; C07B57/00; A61K31/439; A61P13/02; A61P13/10; C07B61/00
Foreign References:
| WO2008062282A2 | 2008-05-29 | |||
| WO2011048607A1 | 2011-04-28 |
Other References:
JPN6015008302; Ｊｏｕｒｎａｌ ｏｆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ ４８, 2005, ６５９７-６６０６
JPN6015008303; Ｔｅｔｒａｈｅｄｒｏｎ ６３（９）, 2007, ４０３９-４０４７
JPN6015008303; Ｔｅｔｒａｈｅｄｒｏｎ ６３（９）, 2007, ４０３９-４０４７
Attorney, Agent or Firm:
Katsunuma Hirohito
Yukitaka Nakamura
Nobutaka Yokota
Yukitaka Nakamura
Nobutaka Yokota