Method for manufacturing of vardenafil and its salts

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United States of America Patent

PATENT NO 9845328
SERIAL NO

15104285

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Abstract

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The method of synthesizing vardenafil base, in anhydrous conditions, by chlorosulfonation of 2-(2-etoxy-phenyl)-5 -methyl-7-propyl-iH-imidazo[5,1-fJ[1,2,4]triazin-4-one in a mixture of thionyl chloride and sulfurochloridic acid followed by amidation of the product, 4-etoxy-3-(5-methyl-4-oxo-7-propyl-3,4-dihydroimidazo[5,1-f][1,2,4]triazin-2-yl)benzene-sulfonic acid chloride with N-ethylpiperazine, in an aprotic solvent, in the presence of an inorganic base and the method of conversion the product, vardenafil base, to yield vardenafil monohydrochloride trihydrate having a melting point of 234° C. by contacting with water of the anhydrous modification V of vardenafil monohydrochloride in an organic solvent. The subject of the invention is also the anhydrous modification V of vardenafil monohydrochloride and its use in the preparation of vardenafil monohydrochloride trihydrate having a melting point of 234° C.

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Patent Owner(s)

Patent OwnerAddress
ZAKLADY FARMACEUTYCZNE POLPHARMA S A83-200 STAROGARD GDANSKI

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Drygas, Jerzy Krotoszyn, PL 2 0
Rynkiewicz, Robert Starogard Gdanski, PL 6 32
Szramka, Roman Gniew, PL 3 1
Szulc, Marcin Starogard Gdanski, PL 2 0

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