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Method for preparing scutellarin and analogues thereof

A technology for scutellarin and its analogues, applied in the field of preparation of scutellarin and its analogues, achieving good bioavailability and flexible reaction routes

Active Publication Date: 2012-10-24
ABIOCHEM BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In addition, the bioavailability of scutellarin needs to be further optimized, and providing suitable scutellarin analogs is expected to solve this problem

Method used

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  • Method for preparing scutellarin and analogues thereof
  • Method for preparing scutellarin and analogues thereof
  • Method for preparing scutellarin and analogues thereof

Examples

Experimental program
Comparison scheme
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Embodiment Construction

[0022] The first aspect of the present invention is to provide a method for synthesizing scutellarin.

[0023] The method for synthesizing scutellarin of the present invention comprises:

[0024] The process of synthesizing 7-OH acceptor compound with naringenin as raw material; the process of synthesizing glucuronic acid donor compound with glucuronic acid 3,6 lactone as raw material; and the acceptor compound and donor compound obtained from the aforementioned process Synthesis of the final product scutellarin.

[0025] The specific synthesis steps are described below.

[0026] Synthesis of 7-OH acceptor compound 11

[0027] The following reaction scheme (A) shows in detail the specific steps for synthesizing the 7-OH acceptor compound represented by structural formula 11 using naringenin represented by structural formula 1 as a raw material.

[0028] Under the action of a catalytic amount of iodine, in the presence of pyridine and under reflux conditions, naringenin 1 u...

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Abstract

The invention discloses a method for preparing scutellarin and analogues thereof. The method comprises the following steps of: preparing a 7-OH receptor compound from naringenin; preparing a uronic acid donor compound from glucuronic acid 3,6 lactone; and reacting the 7-OH receptor compound with the uronic acid donor compound to obtain scutellarin or analogues thereof finally. In the method, naringenin is taken as a raw material, and is cheap and readily available; a reaction route is flexible, and a series of analogues of scutellarin are convenient to obtain; and the obtained analogues of scutellarin have higher bioavailability.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a preparation method of scutellarin and its analogues. Background technique [0002] Scutellarin is a first-line drug widely used clinically to treat cardiovascular and cerebrovascular diseases. It has important pharmacological effects such as expanding cardiovascular and cerebrovascular, increasing blood flow, and improving blood circulation. [0003] The resources of wild scutellarin as a source of scutellarin are limited and are decreasing rapidly year by year. Therefore, it is of great practical significance to develop alternative raw materials and methods for the preparation of scutellarin, especially the efficient large-scale synthesis of scutellaria, which can greatly promote the research and development of traditional Chinese medicine and industrial modernization. [0004] In addition, the bioavailability of scutellarin needs to be further optimized, ...

Claims

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Application Information

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IPC IPC(8): C07H17/07C07H1/00C08G65/48
Inventor 罗煜
Owner ABIOCHEM BIOTECH CO LTD
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