| 摘要 |
NEW MATERIAL:Non-natural type crown dihydrocodein of formula I . USE:A medicament which has combination of properties as opiate and ionophorones. PREPARATION:A thebaine iron complex of formula II is treated with boron tribromide to form a phenol compound, which is then allowed to react with a monotosylate of tetraethylene glycol, then treated with p-toluenesulfonic acid, further 4-dimethylaminopyridine and p-toluenesulfonyl chloride. Then, zinc and acetic acid are used to effect reductive cleavage of the ether ring to give a phenolic compound. Then the product is treated with sodium hydride and trimethylamine oxide and catalytically hydrogenated in the presence of a rhodium complex catalyst to give a reduction product of formula III. The product is treated with a mineral acid to give the compound of formula I . |
