| 摘要 |
<p>PURPOSE: 7-carboxymethyloxy-3',4',5-trimethoxy flavone monohydrate, a method for preparing the same and use thereof are provided, which monohydrate has a protective activity for stomach and intestines and no water absorption, so that the monohydrate can be easily handled and stored under the common room humidity condition. CONSTITUTION: The 7-carboxymethyloxy-3',4',5-trimethoxy flavone monohydrate represented by formula (1) is provided. The method for preparing the 7-carboxymethyloxy-3',4',5-trimethoxy flavone monohydrate represented by formula (1) comprises the steps of: (1) reacting a compound of formula (3) with a methylation reagent in the presence of base, and acid treating the reaction product to prepare a compound of formula (4); (2) reacting the compound of formula (4) with carboxy-protected alpha-haloacetate in the presence of base to prepare a compound of formula (5); (3) reacting the compound of formula (5) with the methylation reagent to prepare a compound of formula (6); and (4) deprotecting the compound of formula (6) and stirring the deprotedted compound in medium containing water, wherein R' is a protecting group, and is ethyl, methyl, t-butyl, benzyl, trichloroethyl or sillyl; the base is selected from potassium carbonate, sodium hydroxide, potassium hydroxide and sodium carbonate; the methylation reagent is methane iodide or dimethyl sulfate; and the acid is hydrochloric acid or sulfuric acid.</p> |
