2,4,5-TRIMETHYLTHIENO (3,2-F)MORPHAN AND PRECURSORS THERETO

摘要

1513980 Tetrahydropyridine derivatives LABORATORIOS MADE SA 25 Aug 1976 [19 Sept 1975] 35397/76 Heading C2C The novel compound of Formula I and salts thereof are prepared by reaction of a compound of Formula II with methyl iodide followed by reduction with NaBH 4 . II may be prepared by hydrazine reduction of a compound of Formula III prepared by reaction of lithiophene with 2- cyano-4,5-dimethyl pyridine obtained by reaction of an alkali metal cyanide with the reaction product of 2,3-dimethylpyridine N-oxide and an alkylating agent. Compounds of Formula I above are cyclized with strong acid to give a compound of Formula IV Pharmaceutical compositions in conventional forms having analgesic activity comprise a compound of Formula I above or a salt thereof or a compound of Formula IV above and a carrier or diluent.