| 摘要 |
1. Process for preparing R- or S-norbenzomorphanes of general formula 1 wherein R<1> may denote H, C1-8alkyl, C1-8alkoxy-, hydroxy or halogen, characterised in that a 4-methylene-piperidine derivative of general formula 2 is converted with an acid into the corresponding acid addition salt and the salt is reacted in a reaction medium with an aluminium (III) halide, preferably aluminium tribromide or aluminium trichloride, at a temperature in the range from 0 to 150 degree C and after the reaction is complete the reaction product is isolated. 2. Process according to Claim 1, characterised in that the reaction medium used is a halogenated aliphatic or aromatic hydrocarbon or an acid amide or mixtures of the aforementioned solvents. 3. Process according to Claim 2, characterised in that the reaction medium used is a mono- or polychlorinated alkane having 1 to 3 carbon atoms, a chlorinated benzene or benzene derivative or an amide of a C1-3-carboxylic acid or mixtures of the abovementioned solvents. 4. Process according to Claim 3, characterised in that the reaction medium used is dichloromethane, 1,2-dichloroethane, chlorobenzene or dimethylacetamide or mixtures of the aforementioned solvents. 5. Process according to one of Claims 1 to 4, characterised in that the reaction is carried out in a temperature range of from 20 to 150 degree C. 6. Process according to Claim 5, characterised in that the reaction is carried out in a temperature range of from 40 to 70 degree C. 7. Process according to one of Claims 1 to 6, characterised in that 2 to 12 equivalents of aluminium (III) halide are used, based on the educt. 8. Process according to clam 7, characterised in that 3 to 10 equivalents of aluminium (III) halide are used, based on the educt. 9. Process according to Claim 8, characterised in that 3 to 5 equivalents of aluminium (III) bromide or aluminium (III) chloride are used, based on the educt. 10. Process according to one of Claims 1 to 9, characterised in that (+)-2-(3-methoxyphenyl)methyl-3,3-dimethyl-4-methylene-piperidine is used as the piperidine derivative. 11. Process according to one of Claims 1 to 9, characterised in that (-)-2-(3-methoxyphenyl) methyl-3,3-dimethyl-4-methylene-piperidine is used as the piperidine derivative. 12. Process according to one of Claims 1 to 10 characterised in that the piperidine derivative is used in the form of an addition salt with a mineral acid. 13. Process according to Claim 12, characterised in that the piperidine derivative is used in the form of an addition salt with a hydrohalic acid or sulphuric acid. 14. Process according to Claim 13, characterised in that the piperidine derivative is used in the form of an addition salt with hydrochloric, hydrobromic or sulphuric acid. |
