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Bicyclic fused heterocyclic compound and preparation method and use thereof

A compound and pharmaceutical technology, applied in the field of medicine, can solve problems such as low cure rate, genotoxicity, and damage

Inactive Publication Date: 2014-08-06
邹宏丽
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chemotherapy is faster, but the cure rate is very low
At the same time, it is clinically found that many anticancer drugs have obvious damage and side effects on the normal body, such as mutagenesis and genotoxicity

Method used

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  • Bicyclic fused heterocyclic compound and preparation method and use thereof
  • Bicyclic fused heterocyclic compound and preparation method and use thereof
  • Bicyclic fused heterocyclic compound and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1: the synthesis of compound 1

[0031]

[0032] Synthesis of compound 1a:

[0033] Dissolve 18.4g (100mmol) of 7-chloro-5-methyl-[1,2,4]triazol[4,3-c]pyrimidin-3-amine in 300mL ethanol, add 10mL85% hydrazine hydrate, room temperature The reaction was stirred vigorously for 14 hours. A white solid was obtained by filtration, washed with ethanol and dried to obtain 18.4 g of white solid compound 1a, with a yield of 95%.

[0034] MS (m / z): 180.10 [M+H] +

[0035] Synthesis of compound 1b:

[0036] Dissolve 17.6g (100mmol) of benzenesulfonyl chloride in 20mL of dichloromethane, cool to 0°C, slowly add 10mL of pyridine dropwise to obtain a clear colorless liquid; then dissolve 14.4g (40mmol) of compound 1a in 200mL of dichloromethane Slowly added to the reaction system, stirred overnight at room temperature. The solvent was recovered under reduced pressure and separated by column chromatography to obtain 5.8 g of white solid compound 1b with a yield of 4...

Embodiment 2

[0046] Embodiment 2: the synthesis of compound 2

[0047]

[0048] The method is the same as in Example 1, except that 1-naphthaldehyde is used instead of benzaldehyde to obtain a light yellow solid. Yield: 72%.

[0049] MS (M / Z): 598.23[M+H] +

[0050] Elemental analysis: theoretical value / measured value, C (60.29 / 60.20), H (5.23 / 5.29), N (21.09 / 21.18), O (8.03 / 7.93), S (5.36 / 5.40).

Embodiment 3

[0051]Embodiment 3: the synthesis of compound 3

[0052]

[0053] The method is the same as in Example 1, except that 4-methylpiperazin-1-amine is used instead of 4-methylpiperidin-1-amine to obtain a white solid. Yield: 70%.

[0054] MS (M / Z): 549.21[M+H] +

[0055] Elemental analysis: theoretical value / measured value, C (54.73 / 54.63), H (5.14 / 5.19), N (25.53 / 25.58), O (8.75 / 8.71), S (5.84 / 5.88).

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Abstract

The invention relates to the field of a drug related to anti-tumor, provides a bicyclic fused heterocyclic compound or pharmaceutically acceptable salts thereof, also provides a preparation method of the bicyclic fused heterocyclic compound or the pharmaceutically acceptable salts thereof, a pharmaceutical composition and application thereof as active ingredient in preparation of anti-tumor drugs for treating small cell lung cancers, breast cancers, liver cancers, colon cancers, malignant gliomas, brain tumors, leucocythemia or pancreatic cancer and the like.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a bicyclic condensed heterocyclic compound, a preparation method thereof, a pharmaceutical composition and an application for preparing antitumor drugs. Background technique [0002] Cancer has become a major chronic disease that seriously endangers human health. According to statistics, there are 9 million people who suffer from cancer every year in the world, and 6 million patients die from cancer. Almost one cancer patient dies every second. The annual incidence of cancer in my country is about 1.2 million, the number of cancer deaths is as high as more than 900,000, and the number of patients waiting for treatment exceeds 1.5 million, and there is an increasing trend year by year. Therefore, cancer has become the second largest killer after cardiovascular disease. Clinically, tumors are treated in three major ways: surgery, radiotherapy, and chemotherapy. Altho...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/519A61K31/5377A61K31/55A61P35/00A61P35/02
CPCC07D487/04
Inventor 马宝花王宏徐辉
Owner 邹宏丽
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