Method for preparing phosphate of toluylene compounds containing phenol hydroxyl group

Abstract

The invention disclose a preparation method of phosphate ester of stilbene compound which contains phenolic hydroxyl group, wherein phosphoryl halide intermediate is hydrolyzed in acid condition to obtain relative phosphate to be reacted with alkali to obtain relative phosphate ester. The invention is characterized in simple operation, low cost, mild reaction condition, non inorganic slat remain,high product purity and high yield. The invention uses environment-friend solvent which is recovered easily, with little environment pollution and industrialization production suitability.

Description

technical field The invention relates to the field of medicine and chemical industry, in particular to a method for preparing a phosphate ester salt of a stilbene compound containing a phenolic hydroxyl group. Background technique The phosphate ester salt of the stilbene compound containing phenolic hydroxyl group is a class of water-soluble prodrug, has good clinical application prospect, and its general formula is as shown in formula (1): Formula 1) Wherein the double bond can be Z formula or E formula; R 1 , R 2 , R 3 Any two of them are CH 3 O, another for CH 3 O or H; R 4 for CH 3 O or H; M 1 means H or M 1 = M 2 ,M 2 means K + 、Na + or NH 4 + . The parent compound of the phosphate ester salt of the phenolic hydroxyl-containing stilbene compound is a multi-substituted stilbene natural product or derivative containing a phenolic hydroxyl group with a cis or trans configuration, and its general formula is such as formula (2) Shown: Formula (2) Wher...

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Problems solved by technology

However, the synthesis steps of the above-mentioned preparation methods 1 and 2 are long, the operation is cumbersome, the reagents used are expensive, and the cost is high, so they are not suitable for large-scale industrial production; in the target compound prepared by the preparation method 3, it contains a relatively large amount of inorganic Salt and excessive inorganic alkali, and difficult to remove, have a great impact on product quality

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