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Synthesizing method and use of bone-targeted antiphlogistic medicament

A reaction and compound technology, applied in the field of medicine, can solve problems such as affecting drug absorption, low solubility, and limiting clinical application.

Inactive Publication Date: 2009-07-08
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Rhein in the present invention affects drug absorption due to problems such as low solubility, thereby limiting its clinical application

Method used

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  • Synthesizing method and use of bone-targeted antiphlogistic medicament
  • Synthesizing method and use of bone-targeted antiphlogistic medicament
  • Synthesizing method and use of bone-targeted antiphlogistic medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1: Synthesis of 4,5-diacetyl-anthraquinone-2-acid-2'-hydroxyethyl ester (I-1); (4,5-diacetyl-anthraquinone-2-acid-2 '-hydroxyethyl ester)

[0053] Step a: Add 50 ml of dry dichloromethane, 2.0 g (9.693 mmol) of DCC and 10 drops of dry DMF into a 100 ml eggplant-shaped bottle, and stir at room temperature for 0.5 hours. Afterwards, 2 g (5.435 mmol) of diacetylrhein was added, stirred and reacted at 30° C. for 1 hour, and then all the solvent was distilled off under reduced pressure to obtain the acid chloride. Step b: In a 250ml three-necked bottle, add 50ml of dry ethylene glycol and 1.3ml (9.250mmol) of dry triethylamine. Dissolve the acid chloride prepared in the previous step in about 150ml of dry dioxane, and slowly add it dropwise into a three-necked bottle at room temperature. After the drop is complete, stir at room temperature for 0.5 hour.

[0054] Post-treatment: Add about 2-3ml of water to the reaction solution to stop the reaction, and distill off ...

Embodiment 2

[0057] Example 2: Synthesis of 4,5-diacetyl--anthraquinone-2-acid-2'-(2-hydroxyethoxy) ethyl ester (I-2)

[0058] Step a: In a 100ml eggplant-shaped bottle, add 50ml of dry dichloromethane, 20.0g (96.93mmol) of DCC and 10 drops of dry DMF, and stir at room temperature for 0.5 hours. Afterwards, 2 g (5.435 mmol) of diacetylrhein was added, stirred and reacted at 30° C. for 1 hour, and then all the solvent was distilled off under reduced pressure to obtain the acid chloride. Step b: In a 250ml three-necked bottle, add 50ml of dry diethylene glycol and 1.5ml of dry pyridine. Dissolve the acid chloride prepared in the previous step in about 150ml of dry dioxane, and slowly add it dropwise into a three-necked bottle at room temperature. After the drop is complete, stir at room temperature for 0.5 hour.

[0059] Post-treatment: Pour the reaction solution into about 100ml of ice water, extract with dichloromethane, wash with saturated aqueous sodium chloride solution, and dry over a...

Embodiment 3

[0062] Example 3: Synthesis of 4,5-diacetyl-anthraquinone-2-acid-2'-(2-(2-hydroxyethoxy)ethoxy)ethyl ester (I-3)

[0063] Step a: In a 100ml eggplant-shaped bottle, add 10ml of dry dichloromethane, 2.0g (9.693mmol) of DCC and 10 drops of dry DMF, and stir at room temperature for 0.5 hours. Afterwards, 2 g (5.435 mmol) of diacetylrhein was added, stirred and reacted at 90° C. for 1 hour, and then all the solvent was distilled off under reduced pressure to obtain the acid chloride. Step b: In a 250ml three-necked bottle, add 50ml of dry triethylene glycol and 1.5ml of dry pyridine. Dissolve the acid chloride prepared in the previous step in about 50ml of dry THF, and slowly add it dropwise into a three-necked bottle at room temperature, after the drop is complete, stir at room temperature for 2.5 hours.

[0064] Post-treatment: Pour the reaction solution into about 100ml of ice water, extract with dichloromethane, wash with saturated aqueous sodium chloride solution, and dry ov...

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Abstract

The invention discloses a bone-targeted anti-inflammatory agent, a synthesis method and application thereof, and in particular relates to compounds having a structure in a formula (II), wherein R1 or R2 respectively independently refers to hydrogen or acyl between C1 and C8; R3 refers to aspirin, ibuprofen, naproxen, indometacin or carboxyl residue of diclofenac; and n refers to an integer between 1 and 10. The application of the compounds is to prepare the bone-targeted antiinflammatory agent, in particular medicines for treating osteoarthritis or rheumatic arthritis.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a class of anthraquinone bone-targeted anti-inflammatory drugs, a preparation method and uses. Background technique [0002] Osteoarthritis is a common clinical refractory chronic degenerative disease. In the world, about 9.6% of men and 18.0% of women over the age of 60 have symptoms of osteoarthritis. 80% of osteoarthritis patients have limited activities, and 25% of osteoarthritis patients cannot complete the main daily activities independently, which brings a heavy burden to the family and society. Rheumatoid arthritis is a systemic disease mainly invading the joint synovium, and the incidence rate in autoimmune diseases is 1%-2%. Deformities, etc., seriously affect the life of patients. The traditional drugs for treating arthritis are mainly analgesics and non-steroidal anti-inflammatory drugs (NASIDs); however, long-term application can cause severe gastroduodenal and...

Claims

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Application Information

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IPC IPC(8): C07C69/95C07C67/08A61K31/235A61P29/00A61P19/02
Inventor 吉民段艳冰余佳
Owner SOUTHEAST UNIV
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