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Benzylisoquinoline non-depolarization muscle relaxant, and preparation method and use thereof

A technology of solvent and mivacurium chloride, which is applied in organic chemistry, pharmaceutical formulations, muscular system diseases, etc., can solve the problems of complex preparation process, poor stability, easy degradation, etc., and achieve simple preparation process, good stability, and reproducible good sex effect

Pending Publication Date: 2018-12-04
SICHUAN CREDIT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to solve the problems that the mivacurium chloride product existing in the prior art is easy to degrade, poor in stability, low in purity, strong in hygroscopicity, and complicated in preparation process, and to provide a product with stable properties, high purity, few impurities, and hygroscopicity. Mivacurium chloride hydrate with low, stable water content, simple preparation process, and easy operation control, suitable for large-scale industrial pharmaceutical production

Method used

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  • Benzylisoquinoline non-depolarization muscle relaxant, and preparation method and use thereof
  • Benzylisoquinoline non-depolarization muscle relaxant, and preparation method and use thereof
  • Benzylisoquinoline non-depolarization muscle relaxant, and preparation method and use thereof

Examples

Experimental program
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Effect test

preparation example 1

[0066] Weigh 250g 6,7-dimethoxy-2-(3-hydroxypropyl)-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl]-1,2 , 3,4-tetrahydroisoquinoline chloride, add 6L of 1,2-dichloroethane, and heat to 70°C to dissolve. Add 50 g of (E)-4-octenedoyl chloride, stir the reaction at room temperature for 19 hours, and concentrate under reduced pressure to remove the solvent. Add 2.5 L of chloroform to the obtained residue to dissolve, extract three times (3×3.5 L) with 5% sodium chloride solution, and concentrate the organic phase under reduced pressure to obtain solid mivacurium chloride.

[0067] Preparation of Mivacuronium Chloride Hydrate I

Embodiment 1

[0069] Take 20 g of mivacuronium chloride obtained in Preparation Example 1, add 40 mL of methanol, and heat to 60° C. to dissolve under stirring to obtain a mivacuronium chloride solution. The obtained mivacurium chloride solution was slowly added into 600 mL of diethyl ether, and the stirring was continued at room temperature until no solid was precipitated, then the temperature was lowered to 15° C. and the stirring was continued for 2 hours. After filtration, the filter cake was dried under reduced pressure at 60° C. for 8 hours to obtain 18.7 g of white solid, with a yield of 93.5% and a purity of 95.0%.

[0070] Structure Determination of Mivacurium Chloride Hydrate I:

[0071] (1) thermal analysis: get the white solid of embodiment 1 gained and carry out TGA (thermogravimetric analysis) and DSC (differential scanning calorimetry) test, gained result is respectively as follows figure 1 and figure 2 shown.

[0072] Thermal analysis results show that the white solid ...

Embodiment 2

[0083] Take 20 g of mivacuronium chloride obtained in Preparation Example 1, add 30 mL of dichloromethane, and heat to 35° C. to dissolve under stirring to obtain a mivacuronium chloride solution. The obtained mivacurium chloride solution was slowly added into 400 mL of methyl tert-butyl ether, and stirring was continued at room temperature for 5 hours. After filtration, the filter cake was dried under reduced pressure at 30° C. for 8 hours to obtain 18.84 g of white solids with a yield of 94.2% and a purity of 95.23%. The water content of the product was 3.15% by weight.

[0084] The test results such as thermal analysis, elemental analysis, loss on drying, and moisture determination of the resulting product show that what the present invention obtains is Mivacurium Chloride Hydrate I.

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Abstract

The invention provides a mivacurium chloride hydrate including mivacurium chloride hydrate I and mivacurium chloride hydrate II, and a preparation method and use thereof. The water content of the mivacurium chloride hydrate I is 2.90-3.35 wt%. The mivacurium chloride hydrate disclosed by the invention is good in stability under the conditions of high temperature, high humidity, illumination and acceleration tests; the moisture content is not obviously increased under the condition of a hygroscopicity test, and the product can be stably stored for a long time; and in addition, the preparation process is simple, no special equipment requirement is required, the product is high in yield and purity, the reproducibility is good and the product is suitable for industrial production.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, in particular to mivacuronium chloride hydrate including mivacuronium chloride hydrate I and mivacuronium chloride hydrate II, and a preparation method and use thereof. Background technique [0002] Since the concept of an ideal muscle relaxant was proposed clinically, it has become an important topic in the field of anesthesia to find a non-depolarizing muscle relaxant that has a rapid onset of action, rapid recovery, and no accumulation. Mivacurium chloride, also known as Mevasone, is a benzylisoquinoline short-acting non-depolarizing neuromuscular blocking drug, and it is a new type of ideal muscle relaxant discovered in recent years. Short-acting nondepolarizing muscle relaxants. Its structural formula is as follows: [0003] [0004] Mivacurium chloride was developed by Abbott lab and launched in the United States in 1992. Because it has an ester structure, it can be rapidly ...

Claims

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Application Information

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IPC IPC(8): C07D217/20A61K31/4725A61P21/02
CPCC07D217/20Y02A50/30
Inventor 宿磊李晓莉陈刚傅霖
Owner SICHUAN CREDIT PHARMA
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