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Synthetic method for oroxylin A

A technology of melaleuca paper element and synthesis method, applied in the direction of organic chemistry, etc., can solve the problems of harsh reaction conditions, cumbersome steps, time-consuming and so on

Active Publication Date: 2018-08-28
CHIA NAN UNIV PHARMACY & SCI
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Problems solved by technology

[0010] The steps of the aforementioned chemical synthesis method are relatively cumbersome, and the reaction conditions are also relatively harsh, while the use of biotransformation methods has the problem of time-consuming (6 days)

Method used

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  • Synthetic method for oroxylin A
  • Synthetic method for oroxylin A
  • Synthetic method for oroxylin A

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Embodiment Construction

[0024] refer to figure 1 , an embodiment of the synthesis method of paperlanin A of the present invention, comprising a methylation step 21 and a protecting group removal step 22 .

[0025] In the methylation step 21, baicalin is used as a starting material, and the starting material is subjected to a methylation reaction in a first reaction solution composed of an inorganic base and a methylating reagent, so that 6 of the starting material is -Hydroxyl is methylated to give an intermediate.

[0026] It is well known to those skilled in the art that flavonoids (such as the structure of melaleucain A in this case) have a γ-pyrone ring that is easily cleaved under alkaline conditions. Therefore, generally in the process of synthesizing flavonoids or When utilizing flavonoids to react, all need to be under relatively severe conditions (for example, the reagents used need to remove water, and the reaction should be carried out under inert gas), so as to avoid the γ-pyrone ring in...

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Abstract

The invention provides a synthetic method for oroxylin A. According to the invention, baicalin is used as a starting material, and oroxylin A can be synthesized by using a simple and effective chemical synthesis method.

Description

technical field [0001] The invention relates to a method for synthesizing Oroxylin A, in particular to a method for synthesizing Oroxylin A using baicalin as a starting material. Background technique [0002] Oroxylin A (Oroxylin A), the structure shown in the following formula (I), is a kind of flavonoids, also known as oroxylin or oroxylin, mainly exists in Scutellaria baicalensis Georgi and Oroxylin ( Oroxylumindicum). Melaleucain A has a wide range of physiological activities, such as blood pressure reduction, anti-tumor, neuroprotection, anti-inflammation, etc. Therefore, it is also valued by modern pharmacological research institutes. [0003] [0004] Melaleucain A can generally be extracted from plants such as Scutellaria baicalensis, Orchid Butterfly, Capparis spinosa, Ardisia crispa or Eucommia ulmoides Oliver. However, the extraction method is not only cumbersome and costly, but also has a low yield. Therefore, at present, there are many literatures publishe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/30
CPCC07D311/30
Inventor 李冠汉何文岳王嘉骏
Owner CHIA NAN UNIV PHARMACY & SCI
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