Lek, Tovarna, Farmacevtskih in Kemicnih . . .

Lek, Tovarna Farmecevtskih in Kemicnih Izdelkov

Alenka Jeriha

Anton Copar

Borut Furlan

There is disclosed a process for the preparation of 3-ethyl 5-methyl (.+-.) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyri dine-dicarboxylate monobenzenesulphonate (amlodipine benzenesulphonate) of formula ##STR1## wherein 3-ethyl 5-methyl (.+-.) 2-[2-(N-tritylamino)-ethoxymethyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl -3,5-pyridinecarboxylate is reacted with benzenesulphonic acid in a methanolic or an aqueous methanolic medium at a temperature from 20.degree. C. to the reflux temperature and the title compound is isolated and purified. Amlodipine benzene sulphonate is a valuable anti-ischaemic and anti-hypertensive agent.

Process for the preparation of amlodipine benzenesulphonate

There is disclosed a process for the preparation of 3-ethyl 5-methyl (.+-.) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyri dine-dicarboxylate monobenzenesulphonate (amlodipine benzenesulphonate) of formula ##STR1## wherein 3-ethyl 5-methyl (.+-.) 2-[2-(N-tritylamino)-ethoxymethyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl -3,5-pyridinedicarboxylate is reacted with benzenesulphonic acid in a methanolic or an aqueous methanolic medium at a temperature from 20.degree. C. to the reflux temperature and the title compound is isolated and purified. Amlodipine benzene sulphonate is a valuable anti-ischaemic and anti-hypertensive agent.

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Ljubljana-Polje, Slovenia

Alenka Jeriha