Process for the preparation of amlodipine benzenesulphonate

Details Process for the preparation of amlodipine benzenesulphonate Process for the preparation of amlodipine benzenesulphonate

1994-08-25

1995-08-01

Fan, Jane

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D21186

Patent

active

054381452

ABSTRACT:
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.

REFERENCES:
patent: 4572909 (1986-02-01), Campbell et al.
patent: 4879303 (1989-11-01), Davison et al.

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