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Preparation process of bupivacaine hydrochloride

A kind of technology of bupivacaine hydrochloride and preparation process, which is applied in the production field of bupivacaine hydrochloride, can solve the problems of high production cost, large amount of DMF usage, difficulty in recycling, etc., and achieve the reduction of three wastes, production cost, and Effects of Environmental Pollution

Inactive Publication Date: 2016-11-16
JIANGSU TIANHE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of the preparation method reported in the literature is that the DMF usage is large, the recovery is difficult, and the production cost is high

Method used

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  • Preparation process of bupivacaine hydrochloride
  • Preparation process of bupivacaine hydrochloride
  • Preparation process of bupivacaine hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Add 500g of toluene to a 1L four-necked reaction flask, then add 100g of starting materials, then add 1.01 to 1.05 times the equivalent of anhydrous potassium carbonate, then add 2% to 6% of tetrabutylammonium bromide, and then add 1.1 to 1.3 times the equivalent of n-bromobutane, slowly heat up to 80-85°C, keep the temperature for 5 hours, cool down to room temperature, filter, transfer the filtrate to a 1L four-necked flask, and pass hydrogen chloride gas into the filtrate until no longer Filter until absorbed, wash the filter cake with toluene, and dry to obtain 132.84-141.70 g of bupivacaine hydrochloride, with an HPLC content of >99% and a yield of 90%-96%.

Embodiment 2

[0027] Add 500g of toluene to a 1L four-necked reaction flask, then add 100g of starting materials, then add 1.01 to 1.05 times the equivalent of anhydrous sodium carbonate, then add 2% to 6% tetrabutylammonium bisulfate, and then add 1.1 to 1.3 times the equivalent of n-bromobutane, slowly heat up to 80-85°C, keep the temperature for 10 hours, cool down to room temperature, filter, transfer the filtrate to a 1L four-necked flask, slowly heat up to 80-85°C, add 160g 10% hydrochloric acid solution, stir to form salt, keep warm at 80-85°C and let it stand for stratification. The water layer is divided into a 500ml four-neck flask while it is hot, cool down to 5-10°C to crystallize, filter, and dry the filter cake to obtain bupika hydrochloride. Because 120.82~126.78g, HPLC content>99%, yield 81%~85%.

[0028] From figure 1 It can be concluded that the purity of bupivacaine hydrochloride directly obtained in Example 1 can reach more than 99.7%, and the purity is relatively high....

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Abstract

The invention discloses a preparation process of bupivacaine hydrochloride. According to the specific scheme, N-(2,6-xylyl)-2-piperidine formamide is adopted as a starting raw material and dissolved in methylbenzene, then a deacidification agent, a phase transfer catalyst and bromobutane are added, certain temperature is kept for reacting, and after the reaction is finished, filtering is carried out at room temperature, and a bupivacaine solution is obtained; the bupivacaine solution is acidized with an acidification agent, aftertreatment is carried out, and bupivacaine hydrochloride is obtained through drying. According to the preparation process, the solvent can be recycled, the production cost can be reduced, environmental pollution can be reduced, meanwhile, byproducts of other products of the company are fully utilized, refuse reclamation is achieved, and generated waste gas, waste water and industrial residues are reduced.

Description

technical field [0001] The invention relates to the technical field of production of bupivacaine hydrochloride. Background technique [0002] Bupivacaine hydrochloride is an amide-type local anesthetic generally used for nerve block anesthesia, local infiltration anesthesia and epidural anesthesia. Its mechanism of action is similar to that of amide-type local anesthetics, that is, the drug is first combined with plasma proteins, metabolized by the liver, and then excreted by the kidneys in urine. Its characteristics are: (1) stronger anesthesia (about 4 times that of carbocaine); (2) longer duration (generally about 5 hours, up to more than 10 hours); The respiratory system and circulatory system are less affected; (4) Pregnant women using this product are not easy to spread and affect the fetus. [0003] This product is already a relatively mature product in foreign countries (it has been included in the British Pharmacopoeia in 1973), and the literature reports on its s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/60
CPCC07D211/60
Inventor 王磊刘磊赵云德王志全朱林飞
Owner JIANGSU TIANHE PHARMA CO LTD
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