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Application of 4-amino-pyrrolotriazine derivative in preparation of anti-pulmonary fibrosis preparation

A triazine derivative, pulmonary fibrosis technology, applied in the directions of organic chemistry, drug combination, heterocyclic compound active ingredients, etc. It can solve the problems of poor long-term efficacy and other problems, and achieve the effects of excellent biological activity, short reaction time and simple post-treatment

Active Publication Date: 2020-12-04
TIANJIN QUANHECHENG TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] For a long time, glucocorticoids have been the first choice for the treatment of idiopathic pulmonary fibrosis, especially for the treatment of acute pulmonary fibrosis, but for chronic pulmonary fibrosis less curative effect
In addition, the anti-inflammatory effect of glucocorticoids lasts for a short time, and the long-term efficacy is not good. Clinically, we have been looking for a new way to treat idiopathic pulmonary fibrosis

Method used

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  • Application of 4-amino-pyrrolotriazine derivative in preparation of anti-pulmonary fibrosis preparation
  • Application of 4-amino-pyrrolotriazine derivative in preparation of anti-pulmonary fibrosis preparation
  • Application of 4-amino-pyrrolotriazine derivative in preparation of anti-pulmonary fibrosis preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Example 1: Heptyl 5-methyl-4-(1-aziridine)pyrrolo[2,1-f][1,2,4]triazine-6-carboxylate:

[0069] This embodiment provides a kind of heptyl 5-methyl-4-(1-aziridine)pyrrolo[2,1-f][1,2,4]triazine-6-carboxylate, its synthesis steps as follows:

[0070] 1) Dissolve 1g of 3-methyl-2-cyanopyrrole-4-heptyl carboxylate completely in 6mL of DMF, cool to -25°C, add 0.6gNaH under stirring, and keep stirring at 300r / min for 45min; at 10mL / min Slowly add 150mL of 0.15mol / LNH 2 Cl diethyl ether solution, keep stirring at constant temperature for 2h, raise the temperature to room temperature at 5°C / min and stir for 1h; saturated Na 2 S 2 o 3 After quenching the reaction with an aqueous solution, the organic phase was obtained, the aqueous phase was extracted 3 times with ether, all the organic phases were combined, washed with saturated brine, dried and concentrated over anhydrous sodium sulfate, and separated by silica gel column chromatography (the mobile phase was ethyl acetate: ...

Embodiment 2

[0074]Example 2: Octyl 5-methyl-4-(1-aziridine)pyrrolo[2,1-f][1,2,4]triazine-6-carboxylate:

[0075] This embodiment provides a kind of octyl 5-methyl-4-(1-aziridine)pyrrolo[2,1-f][1,2,4]triazine-6-carboxylate, its synthesis steps With embodiment 1, specifically as follows:

[0076] 1) Dissolve 1.5g of 3-methyl-2-cyanopyrrole-4-octyl carboxylate completely in 9mL of DMF, cool to -22°C, add 0.9gNaH under stirring, and keep stirring at 450r / min for 50min; Slowly add 150mL of 0.16mol / LNH 2 Cl diethyl ether solution, keep stirring at constant temperature for 2h, warm up to room temperature at 4°C / min and stir for 1h; saturated Na 2 S 2 o 3 After quenching the reaction with an aqueous solution, the organic phase was obtained, the aqueous phase was extracted 3 times with ether, all the organic phases were combined, washed with saturated brine, dried and concentrated over anhydrous sodium sulfate, and separated by silica gel column chromatography (the mobile phase was ethyl aceta...

Embodiment 3

[0080] Example 3: Benzyl 5-methyl-4-(1-aziridine)pyrrolo[2,1-f][1,2,4]triazine-6-carboxylate:

[0081] This example provides a kind of benzyl 5-methyl-4-(1-aziridine)pyrrolo[2,1-f][1,2,4]triazine-6-carboxylate, which is synthesized Step is with embodiment 1, specifically as follows:

[0082] 1) Dissolve 2g of 3-methyl-2-cyanopyrrole-4-benzoic acid benzyl completely in 10mL of DMF, cool to -24°C, add 1.2gNaH under stirring, and keep stirring at 360r / min for 60min; Slowly add 150mL of 0.18mol / LNH 2 Cl diethyl ether solution, keep stirring at constant temperature for 2h, warm up to room temperature at 3°C / min and stir for 1h; saturated Na 2 S 2 o 3 After quenching the reaction with an aqueous solution, the organic phase was obtained, the aqueous phase was extracted 3 times with ether, all the organic phases were combined, washed with saturated brine, dried and concentrated over anhydrous sodium sulfate, and separated by silica gel column chromatography (the mobile phase was e...

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Abstract

The invention relates to the technical field of anti-pulmonary fibrosis preparations, in particular to an application of a 4-amino-pyrrolotriazine derivative in preparation of an anti-pulmonary fibrosis preparation, and the 4-amino-pyrrolotriazine derivative has a structural formula shown in the specification, and can prevent and / or treat pulmonary fibrosis diseases induced by common chronic inflammation, infection, environmental agents, radiation, chronic symptoms, medicines, chemical toxicants and the like, effectively inhibits neuraminidase activity in lung tissues, reduces collagen fiber content of the lung tissues, and slows down pulmonary fibrosis lesion development degree, and improves lung immunity, therefore, the product can be used as or used for preparing medicines capable of preventing and / or treating pulmonary fibrosis diseases.

Description

technical field [0001] The invention relates to the technical field of anti-pulmonary fibrosis preparations, in particular to the application of a 4-amino-pyrrolotriazine derivative in the preparation of anti-pulmonary fibrosis preparations. Background technique [0002] Pulmonary fibrosis (PF) is a progressive and fatal diffuse interstitial lung disease characterized by inflammation and extracellular matrix deposition. The cause of most patients with pulmonary fibrosis is unknown (idiopathic). This group of diseases is called idiopathic interstitial pneumonia (IIP), and the most common form of idiopathic interstitial pneumonia (IIP) is pulmonary fibrosis Idiopathic pulmonary fibrosis (IPF) is a severe interstitial lung disease that can lead to progressive loss of lung function. category, with the highest incidence and poor prognosis. Idiopathic interstitial pneumonia (IIP) is divided into the following categories: (1) Common interstitial pneumonia: idiopathic pulmonary fi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61K31/53A61P11/00
CPCC07D487/04A61P11/00
Inventor 宋艳民杨廷全李子凯
Owner TIANJIN QUANHECHENG TECH
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