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Sulfur-containing diphenyl thiazine alkaloids compound and purpose thereof

A technology of dibenzothiazine and alkaloids, which is applied in the biological field of dibenzothiazine, which can solve the problems of poor pain and other problems, and achieve easy storage and transportation, improved operability, and good sliding properties Effect

Inactive Publication Date: 2018-01-16
胡梨芳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Tetrahydropalmatine sulfate (tetrahydropalmatine sulfate) is a dibenzothiazine alkaloid compound. Tetrahydropalmatine has sedative, analgesic, hypnotic, antihypertensive, antiarrhythmic effects, antithrombotic effect of inhibiting platelet aggregation, Anti-senile dementia, inhibit gastric acid secretion, reduce myocardial ischemia-reperfusion injury, reduce cerebral ischemia-reperfusion injury, etc. It is a very low toxicity analgesic and sedative drug, which can partially replace morphine; it is characterized by high safety, It has a good effect on relieving dull pain caused by gastrointestinal system diseases, liver and biliary system diseases; its analgesic effect is weaker than pethidine, but stronger than general antipyretic and analgesic drugs, and has a better effect on chronic persistent pain , less effective on trauma and postoperative pain
In addition to analgesic effect, there are obvious sedative and hypnotic effects

Method used

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  • Sulfur-containing diphenyl thiazine alkaloids compound and purpose thereof
  • Sulfur-containing diphenyl thiazine alkaloids compound and purpose thereof
  • Sulfur-containing diphenyl thiazine alkaloids compound and purpose thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0080] Embodiment 1 tetrahydropalmatine sulfate 1.5 hydrate [(C 21 h 25 NO 4 ) 2 ·H 2 SO 4 1.5H 2 O or C 21 h 25 NO 4 0.5H 2 SO 4 0.75H 2 O] preparation of tetrahydropalmatine 8.1g, add ethanol 50ml in a 250ml flask, stir, heat, add an appropriate amount of 5M sulfuric acid aqueous solution, stir to dissolve, control the solution pH=1.5, continue to stir for about 1 hour, filter , after concentration under reduced pressure, slowly cool to about -20°C, let stand until the precipitate is fully separated, filter, wash the solid with cold ether and cold absolute ethanol, filter with suction, put the obtained solid in a flask, add 2ml of water, Add 1ml of methanol, add an appropriate volume of ethanol and heat to reflux to dissolve all the solids, concentrate under reduced pressure, and place it below -20°C until the crystals are fully separated, filter with suction, dilute the obtained crystals, and dry them with air at about 30°C for 2 hours. Then dry at about 60°C fo...

Embodiment 2

[0081] Embodiment 2 tetrahydropalmatine sulfate 1.5 hydrate [C 21 h 25 NO 4 1 / 2H 2 SO 4 0.75H 2O] preparation of tetrahydropalmatine 8.03g, add ethanol 50ml in a 250ml flask, stir, heat, add an appropriate amount of 5M sulfuric acid aqueous solution, stir to dissolve, control the solution pH=1.5, continue to stir for about 1 hour, filter After concentrating under reduced pressure for a while, add an appropriate amount of isopropanol and place it, slowly cool it to about -20°C, place it until the precipitate is fully separated, filter, wash the solid with cold ether and cold absolute ethanol, and filter it with suction. Put the solid in a flask, add an appropriate volume of 95% ethanol and heat it under reflux to dissolve it, and then concentrate it under reduced pressure for a while, then use about 1ml of isopropanol for recrystallization, and place it below 0°C until the crystals are fully separated. Suction filtration, dilute the obtained crystals, blow dry at about 30°...

Embodiment 3

[0082] Embodiment 3 tetrahydropalmatine sulfate 5 hydrates [(C 21 h 25 NO 4 ) 2 ·H 2 SO 4 ·5H 2 O or C 21 h 25 NO 4 1 / 2H 2 SO 4 2.5H 2 [0] preparation of tetrahydropalmatine 8.51g, add ethanol 50ml in a 250ml flask, stir, heat, add an appropriate amount of 5M sulfuric acid solution, stir to dissolve, control the solution pH=3.0, continue to stir for about 3 hours, filter, After concentrating under reduced pressure for a while, place it aside, add an appropriate amount of isopropanol, slowly cool to about -20°C, place it for three days, filter the precipitated crystals, heat the obtained solid with an appropriate volume of water under reflux, and add an appropriate amount of isopropanol Carry out recrystallization, slowly cool to -20°C and place it for two days, wait for the crystals to be fully separated, filter, dilute the obtained crystals, blow dry at about 25°C for one day, and then dry at about 30°C for about 3 hours to obtain a yellowish solid 4.52 g; melting...

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Abstract

The invention relates to a novel sulfur-containing diphenyl thiazine compound, which has less hygroscopicity and good storage stability, and is suitable for preparing medicines for treating or preventing analgesia, calmness, hypnosis, hypertension, arrhythmia, functional dyspepsia, cough relieving, mental dissociation, drug dependence for heroin, and reverse tumor cells drug resistance, and is capable of delaying or mitigating myocardial Ischemia reperfusion injury, protecting liver, and preventing internal organ infection reaction.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to provide analgesia, sedation, hypnosis, stability, treatment of hypertension, anti-arrhythmia, functional dyspepsia, cough, anti-schizophrenia, detoxification, reversal of drug resistance of tumor cells A dibenzothiazine alkaloid-tetrahydropalmatine sulfate crystalline hydrate that delays or alleviates myocardial ischemia-reperfusion injury and its preparation and use. Background technique [0002] Polymorphic forms of chemical drugs play an important role in drug research. In the field of pharmacology, the research work on drug crystal forms and drug hydrates or drug solvates has been listed in the research scope of the National Twelfth Five-Year Major New Drug Innovation Science and Technology Major Project. Solvents of compounds, including hydrates, have been prepared and used in medicines for a long time, such as the antineoplastic drug cyclophosphamide recorded in the 36th ...

Claims

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Application Information

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IPC IPC(8): C07D455/03A61K31/4375A61P29/00A61P25/20A61P9/12A61P9/06A61P7/02A61P25/28A61P1/04A61P9/10A61P25/00
Inventor 刘力
Owner 胡梨芳
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