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Benzyl-substituted thiazolocyclohexane compounds, and preparation methods and antitumor uses thereof

A compound and hydroxyl technology, applied in organic chemistry, drug combination, antineoplastic drugs, etc., can solve problems such as poor selectivity, low specificity, and multidrug resistance of cancer

Inactive Publication Date: 2015-04-01
ZHEJIANG PHARMA COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are many traditional drugs for the treatment of cancer in our country. They have obvious therapeutic effects in clinical practice, but their disadvantages are: low specificity and poor selectivity, leading to obvious toxic and side effects, and prone to serious cancer multidrug resistance. drug phenomenon

Method used

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  • Benzyl-substituted thiazolocyclohexane compounds, and preparation methods and antitumor uses thereof
  • Benzyl-substituted thiazolocyclohexane compounds, and preparation methods and antitumor uses thereof
  • Benzyl-substituted thiazolocyclohexane compounds, and preparation methods and antitumor uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024]

[0025] Reaction raw materials: commercially available or self-made.

[0026] 1.67g (10mmol) of compound A-1 and 2.75g (10mmol) of compound B-1 were dissolved in 20mL of dry THF, and then 3.04g (30mmol) of Et 3 N, then stirred at room temperature until the reaction was complete (24-48 hours). The reaction mixture was poured into ice water, extracted with 50 mL×3 dichloromethane, the combined organic phases were washed with brine, dried over anhydrous sodium sulfate, and the solvent was evaporated on a rotary evaporator to obtain the crude product of I-1, which was subjected to column chromatography Purification gave the pure product of I-1, white solid, mp.185-187°C; MS, m / z=362 ([M+H] + ).

Embodiment 2

[0028]

[0029] 1.67g (10mmol) of compound A-1 and 2.75g (10mmol) of compound B-1 were dissolved in 20mL of dry THF, then 3.88g (30mmol) of DIPEA was added, and then refluxed with stirring until the reaction was complete (within 10 hours). The reaction mixture was poured into ice water, extracted with 50 mL×3 dichloromethane, the combined organic phases were washed with brine, dried over anhydrous sodium sulfate, and the solvent was evaporated on a rotary evaporator to obtain the crude product of I-1, which was subjected to column chromatography Purification gave the pure product of I-1, white solid, mp.185-187°C; MS, m / z=362 ([M+H] + ).

Embodiment 3

[0031]

[0032] 1.51g (10mmol) of compound A-1 and 2.75g (10mmol) of compound B-1 were dissolved in 20mL of dry THF, then 3.88g (30mmol) of DIPEA was added, and then refluxed with stirring until the reaction was complete (within 10 hours). The reaction mixture was poured into ice water, extracted with 50mL×3 dichloromethane, the combined organic phases were washed with brine, dried over anhydrous sodium sulfate, and the solvent was evaporated on a rotary evaporator to obtain the crude product of I-2, which was subjected to column chromatography Purification gave the pure product of I-2, white solid, mp.216-219°C; MS, m / z=346 ([M+H] + ).

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PUM

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Abstract

The invention relates to the anticancer related medicine field, and concretely relates to thiazolocyclohexane compounds having a structure represented by general formula I and having an antitumor performance, and preparation methods, medicinal compositions and uses thereof. All groups in the formula I are defined in the specification.

Description

technical field [0001] The invention relates to the field of anti-tumor related drugs. Specifically, the present invention relates to thiazolocyclohexane derivatives with antitumor effects, their preparation methods, pharmaceutical compositions containing them and their antitumor application. Background technique [0002] Cancer is the primary disease that threatens human life. According to statistics, the total number of cancer deaths in the world reaches 7 million people every year. In my country, more than 1 million patients die from cancer every year, and it is gradually increasing. It has become the first cause of death in urban population. At present, there are many traditional drugs for the treatment of cancer in our country, and they have obvious therapeutic effects in clinical practice, but their disadvantages are: low specificity and poor selectivity, leading to obvious toxic and side effects, and prone to serious cancer multidrug resistance drug phenomenon. [0...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D277/60A61P35/00A61P35/02
Inventor 郭章华
Owner ZHEJIANG PHARMA COLLEGE
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