6-Keto-morphinans belonging to the 14-hydroxy-series

Details 6-Keto-morphinans belonging to the 14-hydroxy-series 6-Keto-morphinans belonging to the 14-hydroxy-series

1981-07-16

1983-06-28

Rizzo, Nicholas S.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

424260, 546 45, C07D22128, A61K 31485

Patent

active

043906990

ABSTRACT:
6-Keto-hydroxymorphinans having at the 4 position a substituent which is R.sub.1 =H, O lower alkyl, or O lower acyl, and N may be substituted by R.sub.2, which for agonist properties may be lower alkyl, lower alkenyl, cyclopropylmethyl, or phenyl lower alkyl, etc. Additionally, the nitrogen may be substituted by R.sub.2, which is allyl, cyclopropylmethyl, cyclobutylmethyl, dimethylallyl, etc., which function as antagonists to the morphine-like activity of the compound. Such activity is known as antinociceptive.

REFERENCES:
patent: 3914233 (1975-10-01), Mohacsi et al.
Hsu et al., Heterocycles, 1979, 13 (Spec. Issue), 259-61.
Hsu et al., Helv. Chim. Acta, 1980, 63 (7), 2042-5.
Rozwadowska et al., Can. J. Chem., 1980, 58 (17), 1855-9.
Zakrzewski, Chemical Abstracts, vol. 76, 50006w, (1972).
Schmidhammer et al., Helvetica Chimica Acta, vol. 64, No. 8, pp. 2540-2543, (1981).
Zakrzewski (I), Farmacja Polska, vol. 27, No. 9, pp. 695-698, (1971).
Brossi et al., Chemical Abstracts, vol. 95, 187481j, (1981).
Reden et al., J. Med. Chem., vol. 22, No. 3, pp. 256-259, (1979).
Chemical Abstracts, vol. 76, Chemical Subject Index (E-O), Jun. 30, 1972, morphinan, morphinan-6-one.

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