The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jul. 28, 2015

Filed:

Feb. 08, 2013
Applicant:

Hovione International Limited, Wanchai, CN;

Inventors:

Luis Sobral, Loures, PT;

Marcio Temtem, Quinta do Conde, PT;

Rafael Antunes, Setúbal, PT;

Bruna Nunes, Alverca, PT;

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 491/08 (2006.01); C07D 451/14 (2006.01); C07D 451/10 (2006.01);
U.S. Cl.
CPC ...
C07D 451/14 (2013.01); C07D 451/10 (2013.01);
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.


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