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Preparation method for puerarin morphine

A technology of puerarin and morphine, applied in nervous system diseases, organic chemistry, drug combination, etc., can solve problems such as increasing the complexity of drug management, and achieve the effect of reducing addiction and tolerance

Inactive Publication Date: 2015-09-02
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although this medication idea can reduce the dosage of morphine, it increases the complexity of medication management, and at the same time prevents the emergence of new side effects

Method used

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  • Preparation method for puerarin morphine
  • Preparation method for puerarin morphine
  • Preparation method for puerarin morphine

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Embodiment Construction

[0025] The following will clearly and completely describe the technical solutions in the embodiments of the present invention with reference to the accompanying drawings in the embodiments of the present invention. Obviously, the described embodiments are only some, not all, embodiments of the present invention. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention.

[0026] see Figure 1~2, in the embodiment of the present invention, a kind of preparation method of puerarin morphine, comprises the following steps:

[0027] (1) Synthetic steps of puerarin:

[0028] 1) Add 300mL of anhydrous dichloromethane and 27.0g, 50.0mmol of raw material 1 into a 500mL three-neck flask, add 8.8g, 75.0mmol of NMO in batches under stirring, stir for 20min, and then add 0.88g, 2.5mmol of TPAP , continue to stir the reaction at room tempe...

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Abstract

The invention discloses a preparation method for puerarin morphine. The preparation method comprises the following steps: (1) the synthesis of puerarin, to be specific, 1) preparing a compound 2 by taking a compound 1 as a raw material; 2) modifying the compound 2 to prepare a compound 3; 3) removing hydroxide radicals of the compound 3 to prepare a compound 4; 4) enabling the compound 4 to react with p-methoxyphenylacetyl chloride to prepare a compound 5; 5) reducing the compound 5 into a compound 6 through boron tribromide; 6) synthesizing the puerarin by taking the compound 6 as a raw material; (2) the synthesis of puerarin morphine. Through the use of the puerarin morphine, the dosage of morphine is reduced, the addiction and tolerance of the morphine are reduced, side effects of the morphine in the aspects of the respiratory system, cardiovascular system and central nervous system are effectively slowed down, and the puerarin morphine can be used for pain treatment as a substitute for morphine.

Description

technical field [0001] The invention relates to a puerarin morphine, in particular to a preparation method of the puerarin morphine. Background technique [0002] Pain is a common symptom of many diseases. In terms of pain treatment, commonly used clinical drugs mainly include five categories of narcotic analgesics, antipyretic analgesics, antineuralgia drugs, antimigraine drugs and antispasmodic analgesics. Narcotic analgesics produce analgesic effects by stimulating opioid receptors in specific parts of the central nervous system, and can relieve tension and anxiety at the same time. Morphine, as a typical representative of this class of drugs, can relieve pain caused by various causes, and has the characteristics of strong effects, etc., and has been the preferred narcotic analgesic drug widely used in clinical practice. However, long-term use of morphine produces severe tolerance and addiction. In order to solve this problem, existing studies have modified the structu...

Claims

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Application Information

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IPC IPC(8): C07D519/00A61P25/36A61P25/04
CPCC07D519/00
Inventor 王军阳曾晓艳
Owner XI AN JIAOTONG UNIV
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