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Flavonoid derivative as well as preparation method and identification method thereof

An identification method and a derivative technology, which are applied in the field of flavonoid derivatives and their preparation, can solve the problem that the crystal structure of CDK1 has not been reported, and achieve the effects of improving selective inhibition and clear target.

Inactive Publication Date: 2019-01-25
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The crystal structure of CDK1 has not been reported

Method used

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  • Flavonoid derivative as well as preparation method and identification method thereof
  • Flavonoid derivative as well as preparation method and identification method thereof
  • Flavonoid derivative as well as preparation method and identification method thereof

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preparation example Construction

[0058] The present invention also provides a preparation method of flavonoid derivatives, using a compound of general formula (III) to obtain a compound of general formula (IV) after deglucuronidation, and then substituting an aminomethyl group to obtain a compound of general formula ( V) compounds;

[0059] Carry out esterification reaction to the compound with general formula (V) to obtain the compound with general formula (I);

[0060] Carry out etherification reaction to the compound with general formula (V) to obtain the compound with general formula (II);

[0061] Wherein, the compound with general formula (III), general formula (IV) and general formula (V) is:

[0062]

[0063] Among them, R 1 is alkyl or cycloalkyl, R 2 is alkyl or cycloalkyl, R 1 , R 2 and a nitrogen atom to form an alicyclic or heterocyclic ring.

[0064] In another embodiment, R 1 , R 2 and nitrogen atom to form a tetrahydropyrrole ring.

[0065] In another embodiment, R 1 , R 2 and ni...

Embodiment 1

[0079]

[0080] Weigh 4 g of baicalin (compound represented by formula (Ⅲ)) and dissolve it in 20 mL of water to form a paste, slowly add 100 mL of 50% sulfuric acid, mechanically stir in a water bath at 90°C until clear, continue to react for 5 minutes, and pour it into the preparation Prepare 500mL of ice water, then carry out suction filtration under reduced pressure, wash the filter cake with water until nearly neutral, discard the filtrate, dry the filter cake under vacuum for 24 hours, take appropriate amount of ethyl acetate to disperse into a homogeneous suspension, and filter under reduced pressure , the filter cake was washed 3 times with ethyl acetate, and the filter cake was vacuum-dried for 24 hours to obtain 1.74 g of baicalein (compound represented by formula (IV)) with a yield of 71.9%.

[0081] Weigh 1.08g (0.004mol) of baicalein (the compound shown in formula (IV)) in a 150mL reaction flask, add 30mL of methanol as a solvent, and add 0.486mL (0.006mol) of 3...

Embodiment 2

[0089]

[0090] Weigh 4 g of baicalin (the compound represented by formula (III)) and dissolve it in 20 mL of water to form a paste, slowly add 100 mL of 50% sulfuric acid, stir mechanically in a water bath at 90°C until it becomes clear, continue to react for 5 minutes, and pour into the preparation while stirring. 500mL of fresh ice water, then subjected to vacuum filtration, the filter cake was washed with water until nearly neutral, the filtrate was discarded, and after the filter cake was vacuum-dried for 24 hours, an appropriate amount of ethyl acetate was dispersed into a homogeneous suspension, and vacuum filtered. , the filter cake was washed three times with ethyl acetate, and the filter cake was vacuum-dried for 24 h to obtain 1.74 g of baicalein (a compound represented by formula (IV)) with a yield of 71.9%.

[0091] Weigh 1.08 g (0.004 mol) of baicalein (a compound represented by formula (IV)) in a 150 mL reaction flask, add 30 mL of methanol as a solvent, and u...

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Abstract

The invention discloses a flavonoid derivative, which has structure formulas shown as a general formula (I) and a general formula (II) as in the description, wherein R1 is alkyl or cyclo alkane; R2 isalkyl or cyclo alkane; R1, R2 and nitrogen atoms form cycloaliphatic ring or heterocycle; R3 is alkyl or aryl or aralkyl; the value of n is 1 to 10. The invention also discloses a preparation methodand an identification method of the flavonoid derivative.

Description

technical field [0001] The invention relates to research on flavonoid derivatives, in particular to a flavonoid derivative and its preparation method and identification method. Background technique [0002] Malignant tumors are uncontrolled cell regulation caused by gene mutations, and cells proliferate freely and without restriction. Cyclin-dependent kinase 1 (CDK1) combines with cyclin B (Cyclin B) to form a complex. In the absence of other CDK / Cyclin, it can still catalyze substrate phosphorylation and promote cell division process. Therefore, CDK1 has become a potential target for anti-tumor drug research, and research on CDK1 inhibitors has become a new direction for the development of anti-tumor drugs. [0003] The currently developed CDKs inhibitors are mainly ATP competitive inhibitors. Although different CDKs play different roles in cell cycle progression, because of the similarity in the structure of their ATP-binding domains, the early developed CDKs inhibitors ...

Claims

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Application Information

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IPC IPC(8): C07D311/30C07D493/04G01N21/82G01N24/08G01N30/00G01N30/90A61P35/00
CPCA61P35/00C07D311/30C07D493/04G01N21/82G01N24/087G01N30/00G01N30/90
Inventor 牟佳佳陈党辉邓雁如王莉宁王丽莉任晓亮赵启铎葛军
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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