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Pleuromutilin derivative, and preparation method and application thereof

A technology of pleuromutilin and derivatives, which is used in pharmaceutical formulations, medical preparations containing active ingredients, antibacterial drugs, etc.

Inactive Publication Date: 2015-01-28
LANZHOU INST OF ANIMAL SCI & VETERINARY PHARMA OF CAAS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Currently, the only pleuromutilins available are tiamectin, warnimulin and retapamulin

Method used

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  • Pleuromutilin derivative, and preparation method and application thereof
  • Pleuromutilin derivative, and preparation method and application thereof
  • Pleuromutilin derivative, and preparation method and application thereof

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Embodiment Construction

[0037]Preferred embodiments of the present invention are described below, and it should be understood that the preferred embodiments described here are only used to illustrate and explain the present invention, and are not intended to limit the present invention.

[0038] Pleuromutilin derivatives, chemical structural formula such as I or II:

[0039]

[0040] Wherein: wherein: in formula (II) H2N-X is One of.

[0041] A kind of method for preparing above-mentioned compound, at first synthesizing intermediate-14-O-[(2-amino-1,3,4,-thiadiazol-5 base) mercaptoacetyl] Mutilin (compound 4), then Using this intermediate as a raw material, the above-mentioned compounds 5a-c, 6a-d were synthesized, respectively. The reaction scheme is as follows:

[0042]

[0043] Synthesis of 22-O-(4-toluenesulfonyl)oxyacetylmtilin

[0044] 75.7g (0.2mol) of pleuromutilin and 42g (0.22mol) of p-toluenesulfonyl chloride were dissolved in 200ml of methyl tert-butyl ether, and the mixture ...

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Abstract

The present invention belongs to the field of chemical medicines, and concretely relates to a pleuromutilin derivative, and a preparation method and an application thereof. The preparation method of the pleuromutilin derivative includes the following steps: 1, preparing 22-O-(4-tosyl)oxoacetylmutilin powder; 2, preparing 14-O-(iodoacetyl)mutilin; 3, synthesizing 14-O-[(2-amino-1,2,3,4-thiadiazole-5-yl)mercaptoacetyl]mutilin; and 4, synthesizing an end product. The synthesis method of like compounds has the advantages of easily available raw materials, low price, simple operation, easy separation and purification of the product, and high yield, and realizes a total yield of 30-38%.

Description

technical field [0001] The invention belongs to the field of chemical medicines, and in particular relates to pleuromutilin derivatives and their preparation methods and applications. Background technique [0002] The discovery and use of antibiotics is of great significance in human history. But in the past 30 years, the widespread use and even abuse of antibiotics has caused many bacteria to develop increasingly serious drug resistance. Due to the emergence of drug resistance, the curative effect of drugs with better curative effect is reduced or invalid. In particular, drug-resistant bacteria such as Staphylococcus aureus, Streptococcus pneumoniae and Mycobacterium tuberculosis that cause respiratory diseases cause more than two million deaths every year, seriously endangering the human health. [0003] Pleuromutilin (chemical structural formula such as figure 1 Shown) is a natural antibiotic discovered in the 1950s. Studies have shown that this compound and some deri...

Claims

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Application Information

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IPC IPC(8): C07D285/135A61K31/433A61P31/04
CPCC07D285/135
Inventor 尚若锋梁剑平张超衣云鹏刘宇郭志廷郝宝成郭文柱王学红杨珍
Owner LANZHOU INST OF ANIMAL SCI & VETERINARY PHARMA OF CAAS
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