Method for preparing compounds derived from 10 Keto morfinan, which comprises mixing a compound with Ammonium Nitrate and Water.Hidroxilar Said Compound to oxidize Hydroxy compound and then said, because have useful Effects such as analgesia, sedation and Altered Mood.

摘要

The present Invention relates to a process for the preparation of the 10 Keto analogues of morphinans compounds.In the case of compounds that have a 3 - hydroxyl Group protected with the Analogue 3 methyl ether is synthesized by Selective methylation phenolic Group in the presence of Basic damino.When using nalbuphine, morphine or codeine as initiator, the 6 additional hydroxyl Group is protected by acetylation.The Analogue is oxidized selectively protected with Cerium Ammonium Nitrate treatment to obtain 10 - (S) - hydroxy Adduct.In addition, 10 - (S) - hydroxy Adduct is oxidized to 10 coto Analogue.Any Group protector has been added before oxidation is Cleft after oxidation to form 10 - cetomorfinano desired.