Unlock instant, AI-driven research and patent intelligence for your innovation.

Purinamine compound and preparation method thereof

A compound, purine amine technology, applied in the field of pharmaceutical chemical synthesis, can solve the problems of high cancer recurrence rate, toxicity, unsatisfactory treatment effect, etc., and achieve the effect of inhibiting tumor growth

Active Publication Date: 2014-03-19
CHENGDU EASTON BIOPHARMACEUTICALS CO LTD
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For middle and advanced cancer patients, because of the spread or metastasis of cancer cells, the treatment effects of the first two methods, namely surgical resection and radiotherapy, are not satisfactory. Therefore, chemotherapy has become the only effective treatment for middle and advanced cancer patients.
[0003] Traditional drug chemotherapy can not only kill local cancer cells, but also kill systemic metastatic lesions, but it has severe toxicity to normal cells
In addition, during the use of traditional drugs, cancer cells develop drug resistance due to mutations, making the recurrence rate of cancer extremely high

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
  • Purinamine compound and preparation method thereof
  • Purinamine compound and preparation method thereof
  • Purinamine compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The preparation of embodiment 1 intermediate [1,2,4] triazol [1,5-c] pyrimidin-5-amine

[0024]

[0025] Dissolve 100g of 5-chloro[1,2,4]-triazol[1,5-c]pyrimidine in 200ml of saturated ammonia methanol solution, stir at room temperature for 24 hours, remove the solvent by rotary evaporation, and add a small amount of 43.7g of solid [1,2,4]triazol[1,5-c]pyrimidin-5-amine was generated by filtration, the yield was 50%, MS: [M+H] + 136.1.

Embodiment 2

[0026] Example 2 Preparation of intermediate N-(2-chloro-9-methyl-9H-purin-6-yl)-[1,2,4]triazol[1,5-c]pyrimidin-5-amine

[0027]

[0028] At room temperature, 10g of 2,6-dichloro-9-methyl-9H-purine was dissolved in 100ml of absolute ethanol, and 7g of diisopropylethylamine and 7.32g of diisopropylethylamine prepared in Example 1 were added to this solution [1,2,4]triazol[1,5-c]pyrimidin-5-amine, reflux overnight, remove the solvent by rotary evaporation, add cold water to the residue to form a solid, filter, and dry in vacuo to obtain N-(2- Preparation of chloro-9-methyl-9H-purin-6-yl)-[1,2,4]triazol[1,5-c]pyrimidin-5-amine 12g, 81% yield, MS, m / Z: [M+H] + 302.7.

Embodiment 3

[0029] Example 3 Intermediate N-(2-chloro-9-methyl-9H-purin-6-yl)-N-methyl-[1,2,4]triazol[1,5-c]pyrimidine-5 - Preparation of amines

[0030]

[0031] At room temperature, 5 g of N-(2-chloro-9-methyl-9H-purin-6-yl)-[1,2,4]triazol[1,5-c]pyrimidine- 5-Amine was dissolved in 50 ml of DMF, and 2.36 g of potassium carbonate was added to this solution. The reaction solution was cooled to 0°C, 3.53 g of iodomethane was added, and stirred at room temperature for 12 hours. The reaction solution was slowly poured into stirred water, and the resulting solid was filtered and dried to obtain N-(2-chloro-9-methyl-9H-purin-6-yl)-N-methyl-[1,2,4 ] Triazol[1,5-c]pyrimidin-5-amine 5.18g, yield 99%. MS: [M+H] + 316.7.

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 method belongs to the field of pharmaceutical chemistry synthesis, and specially relates to a purinamine compound and a preparation method thereof. Experiments of inhibitory action on tumour growth in Kunming mice with Lewis lung cancer show that the purinamine compound has an obvious effect for inhibiting the tumour growth and can be applied to prepare drugs, especially tumour drugs, for treating high propagation diseases.

Description

technical field [0001] The invention belongs to the field of pharmaceutical chemical synthesis, and in particular relates to a purine amine compound and a preparation method thereof. Background technique [0002] Cancer is one of the most important diseases that seriously threaten human health. At present, the main methods of cancer treatment are divided into three categories: surgical resection, radiotherapy and drug chemotherapy. Surgical resection and radiotherapy are both local therapies, suitable for early-stage cancer patients without metastasis. For middle and advanced cancer patients, because of the spread or metastasis of cancer cells, the treatment effects of the first two methods, namely surgical resection and radiotherapy, are not satisfactory. Therefore, chemotherapy has become the only effective treatment for middle and advanced cancer patients. . [0003] Traditional drug chemotherapy can not only kill local cancer cells, but also kill systemic metastatic l...

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 Patents(China)
IPC IPC(8): C07D473/16C07D519/00A61K31/52A61P35/00
Inventor 王颖李建国肖雯
Owner CHENGDU EASTON BIOPHARMACEUTICALS CO LTD