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US 8,008,495 B2Granted
Method for preparing tiotropium salts
AssigneeBoehringer Ingelheim Pharma GmbH & Co. KG
InventorsRalf Lock, Werner Belzer, Rainer Hamm, Monika Hofmann
Life of this patent
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Abstract
The invention relates to a new process for preparing tiotropium salts of general formula 1 wherein X− may have the meanings given in the claims and in the specification.
Claims2
A compound of formula 3
- wherein
- R is a group selected from N-imidazolyl, N-triazolyl, —O—C(═NR′)—NHR″, —O—SO2-phenyl, —O—SO2-phenyl-methyl, —O—SO2—R′—O—CO—C(methyl)3, —O—CO-phenyl-NO2, chlorine, bromine, —N3 and —O—(P═O)R′″, where
- R′ denotes C1-C4-alkyl or C3-C6-cycloalkyl;
- R″ denotes C1-C4-alkyl, C3-C6-cycloalkyl, C1-C4-alkylene-N(C1-C4-alkyl)2;
- R′″ denotes C1-C4-alkyl, —O—C1-C4-alkyl, phenyl or —O-phenyl;
- R1 and R2, which may be identical or different, represent methyl, ethyl, propyl, butyl or phenyl, wherein phenyl may optionally be substituted by one or more C1-C4-alkyl groups.
3 more elements
A compound of formula 4
- wherein
- X− represents an anion with a single negative charge, preferably an anion selected from among chloride, bromide, iodide, methanesulphonate or trifluoromethanesulphonate;
- and
- R1 and R2, which may be identical or different, represent methyl, ethyl, propyl, butyl or phenyl, wherein phenyl may optionally be substituted by one or more C1-C4-alkyl groups.
1 more element
Dependencies are inferred from the claim text.