Benzomorphane derivatives

Details Benzomorphane derivatives Benzomorphane derivatives

C - Chemistry, Metallurgy

07

D

260/237.87

C07D 221/26 (2006.01)

Patent

CA 1074310

BENZOMORPHAN DERIVATIVES ABSTRACT OF THE DISCLOSURE 2-Substituted-2'-methyl-6,7-benzomorphan derivatives of the formula: Image [I] wherein R1 and R2 are each hydrogen or C1-C3 alkyl; and R3 is hydrogen, halogen or C1-C3 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: Image [II] wherein R1 and R2 are as defined above, with a reactive derivative of an alcohol compound of the formula: Image [III] wherein X is an optionally protected carbonyl group; and R3 is as defined above, optionally followed by the elimi- nation of the protective group of the carbonyl group, or by the oxidation of a 6,7-benzomorphan derivative of the formula: Image [IV] wherein R1, R2 and R3 are as defined above.

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