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Method for synthesizing chalcone derivative with anti-malaria activity

A technology of chalcone derivatives and synthetic methods, which is applied in the field of drug synthesis, can solve the serious and fatal problems of falciparum malaria, and achieve the effect of short production cycle and simple operation

Inactive Publication Date: 2018-05-15
杨文思
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If not treated within 24 hours, falciparum malaria can develop into a serious and often fatal disease

Method used

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  • Method for synthesizing chalcone derivative with anti-malaria activity
  • Method for synthesizing chalcone derivative with anti-malaria activity
  • Method for synthesizing chalcone derivative with anti-malaria activity

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Synthesis conditions of 1-(7-hydroxy-2-methyl-2-(4-methylpent-3-en-1-yl)-2H-benzopyran-8-yl)ethan-1-one 2 for:

[0030] Mix 2,6-dihydroxyacetophenone 1 (72g), citral dimethyl acetal (141g) and pyridine (370g) and stir at 100-150°C for 10-15 hours; add ethyl acetate to the system (800mL) and saturated copper sulfate solution (600mL), stirred for 1-2 hours, and the organic phase was separated; n-heptane (1000mL) was added to the organic phase, stirred for 2-5 hours, filtered to obtain 1-(7-hydroxy- 2-Methyl-2-(4-methylpent-3-en-1-yl)-2H-benzopyran-8-yl)ethan-1-one 2 (83 g, 61%).

[0031] 1 H NMR (400MHz, DMSO-d6)δ=16.5(s,1H),7.93(d,1H),6.88(d,1H),6.44(d,1H),5.92(d,1H),5.20(t, 1H),2.54(s,3H),1.94(m,3H),1.82(m,3H),1.70(s,3H),1.62(s,2H),1.24(s,3H)ppm; m / z( MS-ESI):287.35[M+1] + .

[0032](E)-1-(7-Hydroxy-2-methyl-2-(4-methylpent-3-en-1-yl)-2H-benzopyran-8-yl)-3-(6 -methylpyridin-3-yl) prop-2-en-1-one synthesis conditions are:

[0033] 1-(7-Hydroxy-2-methyl-2-(4-methy...

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Abstract

The invention discloses a chalcone derivative (E)-1-(7-hydroxyl-2-methyl-2-(4-methylpentan-1-ol-3-alkene-1-base)-2H-benzopyran-8-base)-3-(6-picoline-3-base) acrylic-2-alkene-1-ketone with anti-malariaactivity and a process for synthesizing the chalcone derivative. The chalcone derivative (E)-1-(7-hydroxyl-2-methyl-2-(4-methylpentan-1-ol-3-alkene-1-base)-2H-benzopyran-8-base)-3-(6-picoline-3-base)acrylic-2-alkene-1-ketone and the process have the advantages that the chalcone derivative is excellent in anti-malaria activity; the chalcone derivative which is a compound can be prepared by the aid of the process which is easy to operate and short in production cycle on a large scale.

Description

technical field [0001] The field of the invention belongs to the field of drug synthesis, in particular to a chalcone derivative (E)-1-(7-hydroxyl-2-methyl-2-(4-methylpent-3-ene) with antimalarial activity -1-yl)-2H-benzopyran-8-yl)-3-(6-methylpyridin-3-yl)prop-2-en-1-one and its synthesis process. Background technique [0002] Malaria is an acute febrile illness caused by parasites of the genus Plasmodium. These parasites are transmitted to humans through the bite of infected female Anopheles mosquitoes, known as "malaria vectors." Five species of parasites cause malaria in humans, of which Plasmodium falciparum and Plasmodium vivax are the most harmful. In non-immune people, symptoms usually appear 10-15 days after being bitten by an infected mosquito. Initial symptoms (fever, headache, and chills) may be mild, making it difficult to detect malaria. If not treated within 24 hours, falciparum malaria can develop into a serious disease that is often fatal. [0003] In 2...

Claims

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Application Information

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IPC IPC(8): C07D405/06A61P33/06
CPCC07D405/06Y02A50/30
Inventor 杨文思
Owner 杨文思
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