专利名称：1, 2, 3, 4, 5, 6-hexahydro-8-hydroxy-2, 6-methano-3-benzazocine derivatives
发明人：ARCHER SYDNEY
申请号：US23977762
申请日：19621123
公开号：US3372165A
公开日：
19680305
专利内容由知识产权出版社提供reactive diluent
摘要：The invention comprises benzazocines (also known as benzomorphans) of the formula in the cis (or normal) form and their salts (including penicillin and ascorbic acid salts), wherein Y is a C3- 5 alkenyl group, a halo-C2- 5-alkenyl group (having one or two chlorine or bromine atoms attached to ethylenic carbon), or a cyano, a cyano-C3- 6-alkenyl, a C3- 5-alkenyl or a C3- 7 cycloalkyl group; R1 is a hydrogen atom or a C1- 4 alkyl group; R2 is a hydrogen atom or a methyl or ethyl group; R3 is a hydrogen atom or a C1-4 alkyl group, and the preparation thereof by either (a) treating the corresponding secondary amine with a compound Y-CH2-An where An is a reactive ester group corresponding to the anion of a strong organic or inorganic acid; or (b) reducing the amide corresponding to the compound of the invention except that Y-CH2 is replaced by Y-CO1 with a reducing agent capable of reducing the CO group to CH2 without affecting any ethylenic linkages, and if desired in either case, forming a salt of the resulting compound; and, where the starting material is an 8-hydroxy compound, if desired, etherifying the hydroxyl group. Pharmaceutical compositions comprises the compounds of the invention (including salts with penicillins, ascorbic acid, barbituric acid) together with an inert carrier or diluent. The compositions are antagonistic towards analgesics and
are also muscle relaxants.
申请人：STERLING DRUG INC.
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