BENZOMORPHAN DERIVATIVES

• Main Authors: HOFFMEISTER F,DT, SCHUBERT H,DT
• Format: Patent
• Language: English
• Published: 15.05.1973
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

1314830 Benzomorphane derivatives BAYER AG 13 May 1970 [17 May 1969] 23212/70 Heading C2C Novel benzomorphan derivatives of the formula and their salts with acids and bases, wherein R is CH 3 , cyclopropylmethyl or cyclobutylmethyl, R1 and R11 are the same or different straight- or branched-chain saturated C 1-5 hydrocarbon radicals, X is -OH, -OR111 or R111 is a straight or branched, saturated or unsaturated C 1-11 hydrocarbon radical, R4 and R5, which can be the same or different, are H or C 1-4 alkyl, or can be linked together either directly or through an oxygen atom to form a heterocyclic ring, A is a bivalent straight or branched, saturated or unsaturated C 1-10 hydrocarbon chain, optionally carrying one or more phenyl substituents which may carry one or more alkyl, alkoxy, halogen, NO 2 or acylamino substituents, may be obtained by reacting a compound of the formula with reactive esters (e.g. halides or tosylates) of compounds of formula Z-A-OH, where Z is -CO-X or CN, and when Z = CN, further converting this into -COX by hydrolysis or by alcoholysis followed by hydrolysis, and optionally converting the product to a salt. The compounds of Formula (I) can also be converted to other compounds of Formula (I) by known methods. Pharmaceutical compositions, useful as analgesics, and, in some cases, for therapy of manicdepressive mental illness, comprise compounds of Formula I above in admixture with a solid or liquid diluent or carrier, in forms suitable for oral or parenteral administration.