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AssigneeLek Pharmaceuticals D.D.
InventorsBorut Furlan, Marijan Resnik
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3-ethyl 5-methyl (+/−) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate, containing overall impurities of significantly less than 0.3% is disclosed, as well as process for its preparation, according to which substance of 3-ethyl 5-methyl (+/−) 2-[2-(N-trialkylamino)ethoxymethyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate is converted with benzenesulfonic acid in ethanol solution, at a temperature between 20° C. and reflux temperature, followed by isolation and purification of 3-ethyl 5-methyl (+/−) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate. Amlodipine benzenesulfonate is useful as an antiishemic and antihypertensive agent.
A process for preparing 3-ethyl 5-methyl (+/−) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate (amlodipine benzenesulfonate) by converting the substance of 3-ethyl 5-methyl (+/−) 2-[2-(N-tritylamino)ethoxymethyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate and benzenesulfonic acid, wherein the converting of substances is performed in ethanol media, at a temperature between 20° C. and reflux temperature, followed by isolation and purification of amlodipine benzenesulfonate.
The use of amlodipine benzenesulfonate, containing overall impurities of significantly less than 0.3%, for the manufacture of a medicament for the treatment of heart diseases or hypertension.
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