500866-00-2

Upstream product

• 528-21-2 2',3',4'-trihydroxyacetophenone 
• 93827-33-9 C₂₉H₂₄O₄ 
• 50439-63-9 1-(2,3,4-tris(benzyloxy)phenyl)ethanone 
• 2652-27-9 1-(3,4-bis(benzyloxy)-2-hydroxyphenyl)ethanone 
• 87-66-1 2-hydroxyresorcinol 

Downstream Products

• 786706-00-1 7,8-bis-(1,1-dimethyl-prop-2-ynyloxy)-2-phenyl-4H-chromen-4-one 
• 786706-01-2 7,8-bis-(1,1-dimethyl-allyloxy)-2-phenyl-4H-chromen-4-one 
• 38183-03-8 7,8-dihydroxyflavone 

Relevant academic research and scientific papers

Method for preparing 7, 8-dihydroxyflavone

A method for preparing 7, 8-dihydroxyflavone relates to a preparation process of (3-pentylphenyl) acetic acid, and comprises the following steps: by taking pyrogallol as a raw material, carrying out Friedel-Crafts reaction with acetyl chloride to prepare 2, 3, 4-trihydroxyacetophenone, selectively protecting 3-and 4-hydroxyl groups by using benzyl chloride, carrying out esterification reaction on the unprotected 2-hydroxyl group and benzoyl chloride, and separating and purifying the 2, 3, 4-trihydroxyacetophenone to obtain 7, 8-dihydroxyflavone. And carrying out Baker-Venkatarman rearrangement, ring closing and debenzylation on an esterification product, so as to obtain the 8-dihydroxy flavone.

Preparation method of 7,8-dihydroxy flavone

The invention relates to a preparation method of 7,8-dihydroxy flavone, and belongs to the technical field of synthesis of medical intermediates. The preparation method comprises the following steps:by taking pyrogallol as a raw material, introducing an acetyl group to synthesize DHF1; protecting three phenolic hydroxyl groups to synthesize DHF2; selectively reducing the ortho-hydroxyl group of the acetyl group to synthesize DHF3; carrying out an aldol condensation reaction on DHF3 and benzaldehyde to prepare DHF4; carrying out a cyclization reaction under the condition of iodine catalysis toobtain DHF5; and finally carrying out a hydrolysis reaction to generate the final product. The method is simple and convenient to operate, reasonable in reaction process, low in production cost, goodin product quality, free of environmental pollution and suitable for industrial production, wherein the content of the product is higher than 98%.

Studies on gambogic acid (IV): Exploring structure-activity relationship with IκB kinase-beta (IKKβ)

Previously we have reported a series of gambogic acid's analogs and have identified a compound that possessed comparable in vitro growth inhibitory effect as gambogic acid. However, their target protein as well as the key pharmacophoric motifs on the target have not been identified yet. Herein we report that gambogic acid and its analogs inhibit the activity of IκB Kinase-beta (IKKβ) through suppressing the activation of TNFα/NF-κB pathway, which in turn induces A549 and U251 cell apoptosis. IKKβ can serve as one of gambogic acid's targets. The preparation of the compounds was carefully discussed in the article. Caged 4-oxa-tricyclo[4.3.1.03,7]dec-2-one xanthone, which was identified as the pharmacophoric scaffold, represents a promising therapeutic agent for cancer and useful probe against NF-κB pathway.