PROCESS FOR PREPARING TIOTROPIUM BROMIDE

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)glyc...

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Main Authors TEMTEM MARCIO, ANTUNES RAFAEL, NUNES BRUNA, SOBRAL LUIS
Format Patent
LanguageEnglish
Polish
Published 30.12.2016
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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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.
AbstractList 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.
Author ANTUNES RAFAEL
NUNES BRUNA
SOBRAL LUIS
TEMTEM MARCIO
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DocumentTitleAlternate Sposób otrzymywania bromku tiotropiowego
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Snippet The present invention relates to a novel process for the preparation of tiotropium bromide there is provided a process for preparing tiotropium bromide...
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HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Title PROCESS FOR PREPARING TIOTROPIUM BROMIDE
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