| 摘要 |
<p>A method of preparation of 4-(2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl)phenol of formula (I), known under the generic name desvenlafaxine, and its pharmaceutically acceptable salts, which comprises (a) stirring up O-benzyl desvenlafaxine or its derivative of formula (II), or its salt, where R is selected from H, 4-methyl, 4-methoxy, 3,4-dimethoxy, 2-nitro, 4-nitro, 4-chloro, 4-bromo, 2,6-dichloro and 2,6-difluoro, in an organic solvent or a mixture of organic solvents, followed by dissolution of the starting substance at pH 3 to 8; (b) transformation of O-benzyl desvenlafaxine or its derivative of formula (II) to desvenlafaxine (I) by catalytic hydrogenation; (c) removing the catalyst from the desvenlafaxine solution with the pH value of 3 to 8 by filtration, followed by increasing pH to a value higher than 8 and lower than 11 by addition of an inorganic or organic base; (d) isolation of desvenlafaxine base (I) by filtration; and (e) transformation of desvenlafaxine base (I) to a pharmaceutically acceptable salt.</p> |
