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Sinomenine derivative

A compound, selected technology, used in the application of anti-inflammatory or antitussive drugs in the treatment of diseases, analgesia, sinomenine derivatives and pharmaceutically acceptable salts thereof, can solve adverse reactions, dosage oversized issues

Active Publication Date: 2012-07-04
赵爱国
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the process of clinical application, adverse drug reactions such as muscle redness and itching have also been discovered one after another, and there is also the problem of excessive dosage

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] Synthesis of Compound 3

[0106]

[0107] Dissolve 3.3g of sinomenine in 100mL of ethyl acetate, then add 1.6g of bromine to the solution, stir at room temperature for 30min, add 20mL of water, transfer to a separatory funnel, shake and mix well, let stand to separate layers, and separate acetic acid Add 2.0 g of boron bromide to the ethyl acetate layer, stir at room temperature for 1 h, filter with suction, recover ethyl acetate under reduced pressure to 25 mL, and crystallize to obtain compound 3 with a yield of 89.52%.

Embodiment 2

[0109] Synthesis of Compound 4

[0110]

[0111] Dissolve 3.3g of sinomenine in 120mL of ethyl acetate, then inject chlorine gas into the solution, stir at room temperature for 30min, add 20mL of water, transfer to a separatory funnel, shake and mix well, let stand to separate layers, and separate ethyl acetate Add 3.2 g of boron bromide to the ethyl acetate layer, stir at room temperature for 1 h, filter with suction, recover ethyl acetate under reduced pressure to 25 mL, and crystallize to obtain compound 4 with a yield of 91.7%.

Embodiment 3

[0113] Synthesis of Compound 2

[0114]

[0115] Dissolve 4.6 g of compound 3 in 30 mL of absolute ethanol, then add zinc powder to the solution, stir at room temperature for 120 min, filter with suction, recover ethanol to 15 mL under reduced pressure, refrigerate at 4°C for 12 h, and crystallize to obtain compound 2 with a yield of 98.2%.

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Abstract

The invention discloses a sinomenine derivative and salt acceptable by pharmacy, and a sinomenine-containing derivative and a drug synthesis of salt acceptable by pharmacy and application thereof. The sinomenine derivative and the salt acceptable by pharmacy are prepared through a chemical synthesis method with sinomenine as a parent compound, have remarkable effects on analgesia, anti-inflammation and relieving cough, are obviously superior to sinomenine, and can be used for curing related diseases.

Description

Technical field [0001] The present invention relates to a compound, in particular to a sinomenine derivative and a pharmaceutically acceptable salt thereof, a preparation method of these compounds or a pharmaceutically acceptable salt thereof, and as an analgesic, anti-inflammatory or antitussive drug in application in the treatment of diseases. Background technique [0002] Sinomenine (sinomenine) is an alkaloid monomer extracted from plants of the family Fangji, and its hydrochloride is mostly used in medicine. Sinomenine has anti-inflammatory, immunosuppressive, analgesic, antihypertensive, anti-arrhythmic and other pharmacological effects. Zhengqing Fengtongning Tablets, Sinomenine Hydrochloride Injection, and Sinomenine Hydrochloride Tablets have been used in clinical practice. Various rheumatic diseases such as rheumatoid arthritis and arrhythmia have achieved good curative effect. However, in the process of clinical application, adverse drug reactions such as muscle...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D221/28C07D401/06C07D413/06A61K31/485A61K31/5377A61P29/00A61P11/14
Inventor 赵爱国
Owner 赵爱国
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