Quercetin derivatives and synthetic method thereof

A synthetic method and technology of quercetin, applied in the field of medicine, can solve the problems of low bioavailability, low biological activity, poor hydrophilicity, etc., and achieve high bioavailability, simple operation, and simple synthesis process conditions Effect

Inactive Publication Date: 2014-04-09
NANCHANG UNIV
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

However, this compound contains multiple polar groups, hydroxyl groups, and its lipophilicity is weak. At the same time, because the hydroxyl groups form hydrogen bonds between molecules, the lattice energy is high, and the hydrophilicity is also poor (the solubility of quercetin in water is 7ug/mL) , quickly absorbed and metabolized into the b

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  • Quercetin derivatives and synthetic method thereof
  • Quercetin derivatives and synthetic method thereof
  • Quercetin derivatives and synthetic method thereof

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Embodiment Construction

[0045] Below in conjunction with specific embodiment, further illustrate the present invention. It should be understood that these examples are only used to illustrate the present invention and are not intended to limit the scope of the present invention. The experimental methods not indicating specific conditions in the following examples are usually in accordance with conventional conditions. All percentages, ratios, ratios, or percentages are by weight unless otherwise indicated.

[0046] Unless otherwise defined, all professional and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art. In addition, any methods and materials similar or equivalent to those described can also be used in the present invention. The preferred implementation methods and materials described herein are for demonstration purposes only.

[0047] The preparation process of the above six preferred compounds of the present invention is as foll...

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Abstract

The invention provides quercetin derivatives. The chemical structural general formulas of the quercetin derivative is as shown in the specification; and the synthetic method of the quercetin derivative comprises the following steps: (1) taking a carbonate and the like as the acid-binding agents and potassium iodide as the catalyst, and reacting the quercetin with a halogen substitute of fatty acid ethyl ester; (2) separating and purifying by silica gelcolumn chromatography, and collecting the same components to obtain three yellow powdery compounds: quercetin ester derivatives; and (3) taking the synthesized derivatives as the reactants, respectively, adding NaOH aqueous solution and taking polyethylene glycol as the phase transfer catalyst; separating and purifying by silica gelcolumn chromatography, and collecting the same components to obtain quercetin carboxylic acid derivatives, respectively. The synthetic method of the series quercetin derivatives provided by the invention is simple and easy to operate; the yield of each product is high; and the series quercetin derivatives are remarkably improved in both water solubility and lipid solubility compared with the quercetin.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a series of quercetin derivatives and a preparation method thereof. Background technique [0002] There are more than 6,000 natural flavonoids found in nature, among which quercetin (3,5,7,3',4'-pentahydroxy flavone) is the most widely existing flavonoid, with about 100 kinds This plant contains quercetin. Numerous scientific research results at home and abroad show that quercetin has a wide range of pharmacological effects and biological activities, such as anti-oxidation and scavenging oxygen free radicals, lowering blood pressure, protecting myocardial ischemia, avoiding ischemia-reperfusion injury, enhancing immune function and anti-cancer, Antibacterial, antiviral and analgesic effects, etc., and quercetin can inhibit the proliferation of human ovarian cancer, breast cancer, white blood cells, and gastrointestinal tumor cells. However, this compound contains mu...

Claims

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Application Information

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IPC IPC(8): C07D311/30
CPCC07D311/30
Inventor 胡蒋宁叶慧邓泽元
Owner NANCHANG UNIV
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