3-ethyl 5-methyl(.+-.)2-[2-(N-tritylamino)ethoxymethyl]-4-(2-chl

Details 3-ethyl 5-methyl(.+-.)2-[2-(N-tritylamino)ethoxymethyl]-4-(2-chl 3-ethyl 5-methyl(.+-.)2-[2-(N-tritylamino)ethoxymethyl]-4-(2-chl

1993-11-10

1995-02-14

Rotman, Alan L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546321, A61K 31455, C07D21186

Patent

active

053896548

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-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.

REFERENCES:
patent: 4572909 (1986-02-01), Campbell et al.
patent: 4879303 (1989-11-01), Davison et al.
USAN and the USP dictionary of drug names, U.S. Pharmacopeial Convention, Inc., (1990), p. 44.

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