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Bisbenzylisoquinoline derivative and preparation and application thereof

A technology of bisbenzylisoquinoline and derivatives, which is applied in the field of medicine and achieves the effects of convenient storage and transportation, improved operability, and good water solubility

Active Publication Date: 2011-04-06
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, the published literature has only reported the bisbenzylisoquinoline compound dimethyl tetrandrine iodide (C 40 h 48 o 6 N 2 I 2 , Molecular Weight: 906.63), so far, there is no public literature report at home and abroad that can be used for non-depolarizing muscle relaxation drugs, that is, bisbenzylisoquinoline compound dimethyltetrandrine iodide crystallization Hydrate [C 40 h 48 o 6 N 2 I 2 ·nH 2 O, n=1.0~4.0] and its preparation method and use

Method used

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  • Bisbenzylisoquinoline derivative and preparation and application thereof
  • Bisbenzylisoquinoline derivative and preparation and application thereof
  • Bisbenzylisoquinoline derivative and preparation and application thereof

Examples

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Embodiment 1

[0051] Example 1 Preparation of dimethyl tetrandrine iodide 3 hydrate Put 3 grams of tetrandrine into a 250ml eggplant-shaped flask, add 100ml of chloroform, heat, stir to dissolve, add 15ml of methyl iodide, control the temperature at 30-80 ℃, stirred for 0.2-3 hours, removed the solvent under reduced pressure, and crystallized the residue with 100ml of ethanol, 5ml of acetone, and 10ml of water, cooled to below 15℃, left to stand until the solid was fully separated out, suction filtered, and dried to obtain Dimethyltetradine iodide crystalline hydrate; recrystallized with 100ml of ethanol, 5ml of acetone, and 10ml of water, cooled to below 15°C, left to stand until the solid was fully separated, filtered with suction, and dried to obtain dimethyltetradine iodide Alkali trihydrate, dry the solid at about 60°C for about 4-5 hours to obtain 2.1g off-white crystals, melting point: 235°C decomposition (uncorrected), [α] D 25 : +179.5°(CH 3 OH, 25mg (dry product) / ml); take the s...

Embodiment 2

[0052] Example 2 Preparation of dimethyl tetrandrine iodide 3.5 hydrate Put 3 g of tetrandrine in a 500 ml round bottom flask, add 100 ml of dichloromethane, heat, stir to dissolve, add 0.35 g of potassium hydroxide while stirring 38% aqueous solution, add 35ml of methyl iodide dropwise under stirring, control the temperature between 20-70°C, stir and react for 2-5 hours, remove the solvent under reduced pressure, and use methanol 30ml, water 100ml, ethyl acetate 2ml , to carry out crystallization, cool the reactant to below 15°C, place it until the solid is fully separated, filter it with suction, recrystallize the crystal with 30ml of methanol, 1ml of ether, and 100-200ml of water, cool it to below 15°C, place it, and wait for the solid to Fully analyze, filter with suction, and dry the obtained crystals at about 40 ° C for about 4 hours to obtain 1.5 g of dimethyl tetrandrine iodide 3.5 crystalline hydrate, melting point: 234 ° C decomposition (ELECTROTHERMAL MELTING POINT A...

Embodiment 3

[0053] Example 3 Preparation of dimethyl tetrandrine iodide monohydrate Put tetrandrine in a 5g 500ml eggplant-shaped flask, add 100ml of methanol and 100ml of dichloromethane, heat, stir to dissolve, add 25ml of iodomethane, control The temperature is between 30-66°C, stirring and reacting for 0.5-4 hours, the solvent is removed under reduced pressure, the residue is crystallized with methanol, isopropanol and water, cooled to below 15°C, and placed until the solid is fully separated, suction filtered, and dried , to obtain dimethyl tetrandrine iodide crystalline hydrate; use methanol, isopropanol and water to recrystallize, cool to below 15°C, and place it until the solid is fully separated out, and then suction filtered. The obtained solid is in the presence of phosphorus pentoxide for 60 ℃ of vacuum drying, obtain dimethyl tetrandrine iodide 1 hydrate 3.1 grams, Karl Fischer's method measures moisture and is 2.29%, thermal analysis: platform weight loss is about 2.15%, and ...

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Abstract

The invention relates to a bisbenzylisoquinoline derivative and preparation and application thereof. The derivative has high storage stability and is suitable for preparing medicaments for treating or preventing muscle relaxation, hypertension, amebic dysentery, antianaphylaxis, antipyresis, analgesis and the like of people and animals.

Description

technical field [0001] The present invention relates to the technical field of medicine, and specifically provides medicines for muscle relaxation, such as bisbenzylisoquinoline derivatives and their preparation and application. Background technique [0002] At present, the published literature only reports the bisbenzylisoquinoline compound dimethyltetrandine iodide (C 40 h 48 o 6 N 2 I 2 , Molecular Weight: 906.63), so far, there is no public literature report at home and abroad that can be used for non-depolarizing muscle relaxation drugs, that is, bisbenzylisoquinoline compound dimethyltetrandrine iodide crystallization Hydrate [C 40 h 48 o 6 N 2 I 2 ·nH 2 O, n=1.0~4.0] and its preparation method and application. Contents of the invention [0003] The present invention relates to bisbenzylisoquinoline derivatives and their preparation and use, and furthermore, relates to muscle relaxants - iodide dimethyltetrandrine derivatives and their preparation and use,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/18A61K31/4748A61P21/02A61P23/00A61P29/00A61P25/04A61P9/12A61P33/04A61P37/08
CPCY02A50/30
Inventor 刘力
Owner 刘力
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