Organic compounds -- part of the class 532-570 series – Organic compounds – Phosphorus esters
Patent
1990-02-26
1991-09-24
Evans, J. E.
Organic compounds -- part of the class 532-570 series
Organic compounds
Phosphorus esters
558 87, C07F 948
Patent
active
050515241
ABSTRACT:
Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R.sup.6, or Z represents a protected or latent amino group Z.degree. and R.sup.4 denotes hydrogen or a hydroxy-protective group R.sup.5, any group R.sup.5 or R.sup.6 is replaced by hydrogen, and/or any group Z.degree. is converted into --NH.sub.2.
REFERENCES:
patent: 3184496 (1965-05-01), Baranauckas et al.
patent: 4064163 (1977-12-01), Drach et al.
patent: 4536355 (1985-08-01), Lee et al.
patent: 4618358 (1986-10-01), Maier
patent: 4656298 (1987-04-01), Dingwall et al.
Phosphorous and Sulfur, vol. 18, pp. 353-356 (1983).
Chemical Abstracts 97:72585v (1982).
Baylis Eric K.
Bittiger Helmut
Frostl Wolfgang
Hall Roger G.
Maier Ludwig
Ciba-Geigy Corporation
Evans J. E.
Villamizar JoAnn
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