Method for preparing ambroxol trans-impurity 6,8-dibromo-3-(trans-4-hydroxycyclohexyl)-1,2,3,4-tetrahydroquiazoline
The invention relates to a novel technology for Febuxostat. The method for preparing the Febuxostat comprises the following steps of: reacting 2-hydroxy-5-cyano-benzaldehyde with NaSH in a solvent to obtain 3-formyl-4-hydroxythiobenzamide; reacting the 3-formyl-4-hydroxythiobenzamide with 2-halogena...
Gespeichert in:
1. Verfasser: | |
---|---|
Format: | Patent |
Sprache: | chi ; eng |
Schlagworte: | |
Online-Zugang: | Volltext bestellen |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | The invention relates to a novel technology for Febuxostat. The method for preparing the Febuxostat comprises the following steps of: reacting 2-hydroxy-5-cyano-benzaldehyde with NaSH in a solvent to obtain 3-formyl-4-hydroxythiobenzamide; reacting the 3-formyl-4-hydroxythiobenzamide with 2-halogenated ethyl acetoacetate, and closing the ring to obtain 2-(3-formyl-4-hydroxyphenyl)-4-methyl-5-ethyoxycarbonylthiazole; reacting 2-(3-formyl-4-hydroxyphenyl)-4-methyl-5-ethyoxycarbonylthiazole with hydroxylamine in a solution of formic acid to obtain 2-(3-cyano-4-hydroxyphenyl)-4-methyl-5-ethyoxycarbonylthiazole; reacting 2-(3-cyano-4-hydroxyphenyl)-4-methyl-5-ethyoxycarbonylthiazole with halogenated isobutene to obtain 2-(3-formyl-4-isobutoxyphenyl)-4-methyl-5-ethyoxycarbonylthiazole under the action of potassium carbonate; and finally, hydrolyzing to remove the ester group by using sodium hydroxide, thereby obtaining the product Febuxostat. The provided preparation method is simple in process and high in reproduc |
---|