Check patentability & draft patents in minutes with Patsnap Eureka AI!

Pyrimidine derivative, synthesis method and applications thereof

A technology of pyrimidine derivatives and pyrimidine, which is applied in the structure of pyrimidine derivatives and the field of preparation thereof, can solve the problems of drug resistance, patient resistance and the like, and achieves the effects of easy operation and simple preparation process.

Active Publication Date: 2020-05-19
TIANJIN UNIV
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Pyrimidine derivative, synthesis method and applications thereof
  • Pyrimidine derivative, synthesis method and applications thereof
  • Pyrimidine derivative, synthesis method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0029] The technical solution of the present invention will be further described below in conjunction with specific embodiments.

[0030]

[0031] 5-chloro-N 4 -(2-(isopropylsulfonyl)phenyl)-N 2 The preparation method of -(2-phenylimidazole[1,2-c]pyrimidin-7-yl)pyrimidine-2,4-diamine is shown in the following chemical reaction process.

[0032]

[0033] Step 1, Preparation of 2-phenylpyrimidine [1,2-c]imidazole-7-amine

[0034] Add 4,6-diaminopyrimidine (110.1mg, 1.00mmol) and methanol (5mL) to a 100mL three-necked flask in turn, magnetically stir to dissolve the raw materials, and then add 2-bromoacetophenone (199.0mg, 1.00mmol), Triethylamine (121.4mg, 1.20mmol) was heated to 55°C, the reaction was stopped after 5h, and cooled to 25°C, a pale yellow solid precipitated, the filtrate was filtered off and a white solid (178.7mg, 85%) was isolated.

[0035] 1 H NMR(500MHz, DMSO-d 6 ), δ: 9.18 (s, 1H), 8.38 (s, 1H), 7.86 (d, J = 7.5 Hz, 2H), 7.57 (t, 2H), 7.50 (t, 1H), 6.50 (s, 2H) ,7.7...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a pyrimidine derivative, a synthesis method and applications thereof. The synthesis method comprises the following steps: obtaining an arylamine compound 2-phenylpyrimidine [1,2-c]imidazole-7-amine, and then carrying out a catalytic coupling reaction on the arylamine compound 2-phenylpyrimidine [1,2-c]imidazole-7-amine and 2,5-dichloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidine-4-amine to obtain the pyrimidine derivative. The preparation method has the advantages that the preparation process is simple and easy to operate. The prepared product has ALK inhibitory activityand can be used for preparing an ALK inhibitor.

Description

Technical field [0001] The invention belongs to the field of medicinal chemistry, and more specifically, relates to the 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 patients with non-small cell lung cancer are already in the advanced stage when they are diagnosed, and the 5-year survival rate is very low. With the deepening of scientific research, scientists have discovered that 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 therapeutic method among many methods for...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61P35/00A61K31/519
CPCA61P35/00C07D487/04
Inventor 周雪琴李巍刘东志韩薇刘路显
Owner TIANJIN UNIV
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com