Laevorotatory antipode of moprolol as an antihypertensive

Details Laevorotatory antipode of moprolol as an antihypertensive Laevorotatory antipode of moprolol as an antihypertensive

1982-10-14

1987-07-28

Schwartz, Richard A.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

564349, A61K 31135

Patent

active

046832459

ABSTRACT:
This invention relates to a process for the separation of moprolol into its two optical antipodes, substantially characterized by the fact of salifying racemic moprolol with L(+)glutamic acid; treating the thus obtained mixture of diastereoisomeric salts with a water/alcohol mixture, in this way separating the L(+)glutamate insoluble salt of (+)moprolol; treating the resultant mother liquors which contain in solution the L(+)glutamate salt of (-)moprolol with a base so as to separate the laevorotatory isomer of crystalline moprolol, which finally undergoes a purification. The invention also relates to a pharmaceutical composition containing said laevorotatoryisomer of moprolol.

REFERENCES:
patent: 3432545 (1969-03-01), Howe
patent: 3483221 (1969-12-01), Wilhelm et al.
patent: 3501769 (1970-03-01), Crowther et al.
patent: 3538150 (1970-11-01), Gilman et al.
patent: 3649691 (1972-03-01), Shavel et al.
patent: 3911136 (1975-10-01), Ferrari
patent: 4131686 (1978-12-01), Ikezaki et al.
Ferrini, R., et al., Arzneim.-Forsch., 20(8), 1074-1079 (1970).
Burger, A. (Editor), Medicinal Chemistry, 3rd Edition, Interscience, New York, 1970, pp. 1052-1055.

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