Title:
A preparing method of bromination tiotropium
Document Type and Number:
Japanese Patent JP6118826
Kind Code:
B2
Abstract:
The present invention relates to a novel process for the preparation of tiotropium bromide there is provided a process for preparing tiotropium bromide comprising (i) reacting scopine oxalate with diethylamine in an inert solvent to form scopine; (ii) reacting scopine and methyl di-(2-dithienyl)glycolate (MDTG) in the presence of an inorganic base, and in an inert solvent to form N-demethyltiotropium; (iii) reacting N-demethyltiotropium with bromomethane in an inert solvent to form tiotropium bromide; (iv) crystallizing tiotropium bromide in a mixture of methanol and acetone, and optionally thereafter, (v) micronizing the tiotropium bromide so formed.
Inventors:
Sobral, Lewis
Tenten, Marjo
Raven, Antonios
Nunis, Bruna
Tenten, Marjo
Raven, Antonios
Nunis, Bruna
Application Number:
JP2014556130A
Publication Date:
April 19, 2017
Filing Date:
February 08, 2013
Export Citation:
Assignee:
Hobione International Limited
International Classes:
C07D451/10
Domestic Patent References:
| JP2008063319A | ||||
| JP5502438A | ||||
| JP2011509284A | ||||
| JP2009519295A | ||||
| JP2005526776A | ||||
| JP2012507483A |
Foreign References:
| CN101863885A | ||||
| WO2011015884A1 |
Attorney, Agent or Firm:
西浦 ▲嗣▼晴
Toshihisa Sakai
High Miki Yoshiki
Tadashi Deyama
Toshihisa Sakai
High Miki Yoshiki
Tadashi Deyama
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