Analgesic benzomorphan derivatives

Details Analgesic benzomorphan derivatives Analgesic benzomorphan derivatives

1976-10-27

1980-12-23

Randolph, John D.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Parasitic organism or component thereof or substance...

546 97, A61K 31445, C07D22126

Patent

active

042410703

ABSTRACT:
2-Substituted-2'-methyl-6,7-benzomorphan derivatives of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sub.3 is hydrogen, halogen or C.sub.1 -C.sub.3 alkyl, and pharmaceutically acceptable salts thereof, which are useful as non-addicting analgesics with sedative effects, are prepared by the reaction of a 6,7-benzomorphan derivative of the formula: ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, with a reactive derivative of an alcohol compound of the formula: ##STR3## wherein X is an optionally protected carbonyl group; and R.sub.3 is as defined above, optionally followed by the elimination of the protective group of the carbonyl group, or by the oxidation of a 6,7-benzomorphan derivative of the formula: ##STR4## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above.

REFERENCES:
patent: 3631051 (1971-12-01), Atsumi et al.
patent: 3632591 (1972-01-01), Albertson et al.
patent: 3833595 (1974-09-01), Atsumi et al.
DeStevens, G. (editor), Analgetics, Academic Press, New York, 1965, p. 163.

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