- AN IMPROVED PROCESS FOR THE PREPARATION OF DARIFENACIN HYDROBROMIDE
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The present invention relates to an improved process for the preparation of Darifenacin hydrobromide of Formula (I). (i) condensing 3-(S)-(-)-1l-carbamoyl-1,1-diphenylmethyl)pyrrolidine (III), or its salt, with a compound of Formula XIII in the presence of a. base in a solvent, wherein X represents Cl, Br, C1-3 alkyl sulfonate or C6-10 arγl sulfonate; to produce (S)-2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]-3- pyrrolidinyl]-2,2-diphenylacetamide (Darifenacin) (Ia), (ix) treating (S)-2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]-3-pyrrolidinyl]- 2,2-diphenylacetamide (Darifenacin) (Ia) with an acid in a solvent and water mixture, (x) isolating pure (S)-2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]-3- pyrrolidinyl]-2,2-diphenylacetamide (Darifenacin) (Ia), (xi) treating pure Darifenacin (Ia) with HBr to produce Darifenacin hydrobromide (I).
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Page/Page column 10-11
(2011/06/26)
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- AMINOCYCLOALKANE COMPOUNDS
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Aminocycloalkane compounds represented by the following general formula: wherein Ar represents a phenyl group or thienyl group with an optional substituent on the ring, X represents a cyano group or carbamoyl group, R1 and R2 are each independent, R1 representing a hydrogen atom or lower alkyl group and R2 representing a hydrogen atom, lower alkyl group, an -A-B group (where A represents a lower alkylene group that is optionally branched and B represents a phenyl group, pyridyl group, thiazole group, imidazole group, furyl group or pyrrolidinyl group with an optional substituent on the ring) or an alkenyl group, or R1 and R2 together with the nitrogen atom to which they are bonded represent (where R3 represents a hydrogen atom, a lower alkyl group that is optionally substituted with a phenyl group, or an alkenyl group), and m represents 2, 3 or 4, and pharmacologically acceptable salts thereof. The compounds have highly selective antagonistic activity for muscarinic M3 receptor subtypes, and are therefore useful as preventive or therapeutic agents for diseases related to muscarinic M3 receptor subtypes.
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