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Pyrimidine-based derivatives and their preparation methods and applications

A technology of derivatives and pyrimidines, which is applied to the structure of pyrimidine derivatives and the field of preparation thereof, can solve the problems of drug resistance of patients and drug resistance, and achieve the effect of simple preparation process and easy operation.

Active Publication Date: 2021-12-24
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, patients who respond to crizotinib often develop resistance to the drug within 1 year of taking it
In recent years, the US FDA has approved a series of ALK inhibitor drugs to treat patients with resistance to crizotinib. However, after a period of medication, patients still develop drug resistance

Method used

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  • Pyrimidine-based derivatives and their preparation methods and applications
  • Pyrimidine-based derivatives and their preparation methods and applications
  • Pyrimidine-based derivatives and their preparation methods and applications

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Embodiment Construction

[0030] The technical solutions of the present invention will be further described below in conjunction with specific embodiments.

[0031]

[0032] 5-Chloro-N 4 -(2-(isopropylsulfonyl)phenyl)-N 2 The preparation method of -(6-phenyl-[1,2,4]triazol[4,3-a]pyridin-3-yl)pyrimidine-2,4-diamine is shown in the following chemical reaction process.

[0033]

[0034] Step 1: Preparation of 6-phenyl-[1,2,4]triazol[4,3-a]pyridin-3-amine

[0035] Add 6-bromo-[1,2,4]triazol[4,3-a]pyridin-3-amine (1.3g, 6.00mmol), phenylboronic acid (877.9mg, 7.20mmol) successively into a 100mL three-necked flask, V (dioxane): V (water) = 15.0: 7.5, cesium carbonate (5.9g, 18.00mmol), magnetic stirring, N 2 0.5h, then add the catalyst bistriphenylphosphine palladium dichloride (421.1mg, 0.60mmol), slowly heat to 80°C, stop the reaction after 8h, add water 50mL, extract 3 times with ethyl acetate, and use anhydrous sulfuric acid It was dried over magnesium and concentrated to obtain a crude solid,...

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Abstract

The present invention discloses derivatives based on pyrimidine and its preparation method and application. Firstly, the arylamine compound 6-phenyl-[1,2,4]triazol[4,3-a]pyridine-3-amine is obtained, and then combined with 2,5-dichloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine is catalyzed to obtain a pyrimidine derivative. The invention has the advantages of simple preparation process and easy operation. The prepared product has ALK inhibitory activity and can be used to prepare ALK inhibitors.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and more specifically relates to a structure of a pyrimidine derivative with ALK inhibitory activity and a preparation method thereof. Background technique [0002] Lung cancer is one of the most common malignant tumors in the world, and its mortality rate ranks first among all malignant tumors. Lung cancer can be divided into non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC), of which 85% belong to non-small cell lung cancer. Most non-small cell lung cancer patients are already in the middle and advanced stages when they are diagnosed, and the 5-year survival rate is very low. With the deepening of scientific research, scientists have discovered that the anaplastic lymphoma kinase (ALK) fusion gene is one of the key genes driving non-small cell lung cancer. [0003] At present, molecular targeted therapy is the most effective and most widely used treatment method among man...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/04A61P35/00
CPCC07D471/04A61P35/00
Inventor 周雪琴李巍刘东志韩薇刘路显
Owner TIANJIN UNIV
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