7,10-Dimethyl-5,9-imino-4,5,8,9-tetrahydro-cyclooct[b]thiophenes and a process for obtaining it
AssigneeLaboratories Made, S.A.
InventorsRicardo Granados Jargue, Mercedes Alvarez Domingo, Juan Bosch Cartes, Cirstobal Martinez Roldan, Fernando Rabadan Peinado
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Abstract
Compounds of the formula: ##STR1## where R is H or lower alkyl and a process for the preparation thereof are disclosed. The compounds are analgesic agents.
Claims5
A process for obtaining 7,10-dimethyl-5,9-imino-4,5,8,9-tetrahydro-cyclooct[b]thiophenes of formula I:
- ##STR3## in which R is H (I,R.dbd.H) or a lower alkyl group, for example methyl (I,R.dbd.CH.sub.3), or the pharmacologically acceptable addition salts thereof, which comprises reacting 3-thienylmagnesium bromide obtained in conditions of high dilution and in inert atmosphere with a N-methyl-pyridinium iodide in anhydrous ether maintained at reflux temperature, with which an unstable dihydropyridine intermediate is obtained which without subsequent purification is treated in acid medium, leading to the formation of the corresponding 7,10-dimethyl-5,9-imino-4,5,8,9-tetrahydro-cyclooct[b]thiophene (I).
A compound selected from the group consisting of 7,10-dimethyl-5,9-imino-4,5,8,9-tetrahydro-cyclooct[b]thiophene and 6,7,10-trimethyl-5,9-imino-4,5,8,9-tetrahydro-cyclooct[b]thiophene or their addition salts with pharmacologically acceptable acids.
A compound of the formula:
- ##STR4## where R is H or lower alkyl or a pharmaceutically acceptable acid addition salt thereof.
Dependencies are inferred from the claim text.