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Separation and purification method of dezocine

A technology for separation and purification of dezocine, applied in organic chemistry methods, chemical instruments and methods, organic chemistry, etc., can solve problems such as danger and acute respiratory depression, and achieve shortened synthesis cycle, improved quality, and mild reaction conditions Effect

Pending Publication Date: 2022-04-22
TAIZHOU DANDING BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It may cause acute respiratory depression after intravenous injection, and it is dangerous to use this product in patients with reduced respiratory reserve

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The present invention provides a separation and purification method of dezocine, which is separated and purified according to organic compounds. The separation and purification method of dezocine comprises the following steps:

[0046] Step 1. Prepare materials and reagents;

[0047] Step 2, sample processing;

[0048] Step 3, separation and purification of dezocine.

[0049] The materials and reagents prepared in step 1 also include: sodium hydroxide, aluminum nickel alloy, ammonia water, dezolone oxime, dezolamide salt, purified water, ethyl acetate, methyl dezocine salt, ethanol, concentrated hydrochloric acid.

[0050] Sample processing in step 2 includes:

[0051] A: The white solid dezolamide salt is prepared and placed in a sterile tank for later use;

[0052] B: Put the refined methyl dezocine salt in a white sterile jar at room temperature for later use;

[0053] C: Cover the methyl dezocine salt and dezolamide salt with a transparent film to keep it clean....

Embodiment 2

[0064] On the basis of Example 1, the present invention provides a technical solution: preferably, the preparation of methyl dezocine salt also includes the following steps:

[0065] B1: In a 120L reaction kettle, add wet methyl dezocine salt essence and 45 times volume of anhydrous methanol;

[0066] B2: Turn on the stirring and heating device, after it is completely dissolved, steam about 80% of anhydrous methanol under normal pressure, turn off the heating device, and put the material into a stainless steel bucket for standby;

[0067] B3: After cooling to room temperature, stand for crystallization for more than 8 hours and then filter to obtain a filter cake, that is, a fine product of wet methyl dezocine salt;

[0068] B4: The filter cake is placed in a vacuum drying oven, and the white crystal is vacuum-dried at about 65°C.

[0069] Purifying dezocine also includes the following steps:

[0070] C1: First, add 800g of dezocine and 20L of ethanol to the reaction kettle;...

Embodiment 3

[0076] On the basis of Example 2, the present invention provides a technical solution: preferably, the storage of purified dezocine also includes the following steps:

[0077] D1: Sterilize the medicinal plastic bag, put the purified dezocine into the medicinal plastic bag and weigh it, and classify the small bags according to the specified weight;

[0078] D2: Fill a certain amount of nitrogen into the medical plastic bag, seal it with a plastic sealing machine, write the production date, use effect, materials and precautions, etc., label it, and put it in a dry area at room temperature.

[0079] Beneficial effects: Through the purification and production of dezocine salt, methyl dezocine salt, dezocine and storage of dezocine, the synthesis steps and reaction conditions are optimized, the synthesis cycle is shortened, the key process parameters and product quality standards are clarified, so that dezocine The dezocine purification process can quickly grasp the key control po...

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PUM

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Abstract

The invention discloses a dezocine separation and purification method, and relates to the technical field of medicine production, separation and purification are carried out according to organic compounds, and the dezocine separation and purification method comprises the following steps: step 1, preparing materials and reagents; 2, carrying out sample treatment; and step 3, separation and purification of dezocine. According to the invention, dezolamide salt, melizocine salt and dezocine are purified and prepared, dezocine is stored, and synthesis steps and reaction conditions are optimized, so that the synthesis period is shortened, the purification preparation route is simple, the steps are few, the yield is high, the operation is simple, the synthesis period is greatly shortened, the reaction conditions are mild, the process safety is improved, the raw material cost is low, and industrialization is facilitated; key process parameters and product quality standards are determined, so that key control points in the dezocine purification process can be quickly mastered, dezocine purification preparation can be efficiently and stably carried out, and convenience is brought to operation.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical production, in particular to a method for separating and purifying dezocine. Background technique [0002] Dezocine is a newly synthesized opioid κ receptor partial agonist with a structure similar to pentazocine, and it is a parenteral analgesic. In animal models, it shows allylmorphine-like antagonism. In animals addicted to morphine, this product can cause withdrawal symptoms; its opioid receptor agonism can be reversed by naloxone. The analgesic effect of intramuscular injection of 10 mg of this product is equivalent to that of 10 mg of morphine or 50-100 mg of meperidine. Onset time and duration of action are similar to morphine. Postoperative use of this product has no significant respiratory depression. Because it stimulates the σ receptor to increase the level of adrenaline in the plasma, it has an exciting effect on the cardiovascular system and can increase the cardiac index, p...

Claims

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Application Information

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IPC IPC(8): C07C213/10C07C213/08C07C215/64
CPCC07C213/10C07C213/08C07C2603/80C07B2200/07C07C215/64
Inventor 顾正兵曾铖沈国亮顾大全李天亭孙春锋
Owner TAIZHOU DANDING BIOTECH CO LTD
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