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Production process of rotundine

A production process, the technology of rotundine, which is applied in the direction of organic chemistry, can solve the problems of secondary injury, high side effects, and short efficacy maintenance time of patients, and achieve the effects of long efficacy maintenance time, reduction of side effects, and improvement of efficacy time

Inactive Publication Date: 2019-02-01
佑华制药(乐山)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The object of the present invention is to provide a kind of rotundine production technology, to solve the problem that the produced rotundine product efficacy maintenance time is short, the side effect is high, and the use of the patient is easy to cause secondary damage to the patient proposed in the above-mentioned background technology

Method used

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  • Production process of rotundine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] This kind of rotundine production technology comprises the steps:

[0027] S1: Manufacture of Schiff's base: Add piperethylamine measured by a balance scale into the condensation tank, add polyoxymethylene under stirring, open the vacuum system to make the vacuum in the tank reach 0.055MPa, and then slowly heat in the interlayer water bath to make the block The methyl-ortho-vanillin is completely dissolved, and the stirring is stopped. Intense foam is produced during the reaction, and the temperature continues to rise. At this time, water droplets can be seen in the cup. When there are no water droplets in the cup, it is the end of the reaction. Continue to keep warm 15.5 minutes, holding temperature 155°C, cooling down to below 60°C, pumping into the autoclave;

[0028] S2: Hydrogenation reaction: pump the catalyst into the autoclave. After all the materials are added, the liquid level reaches the turbine position of the autoclave. After repeated ventilation with hydro...

Embodiment 2

[0041] This kind of rotundine production technology comprises the steps:

[0042] S1: Manufacture of Schiff's base: Add piperethylamine measured by a balance scale into the condensation tank, add polyoxymethylene under stirring, open the vacuum system to make the vacuum in the tank reach 0.05MPa, and then slowly heat in the interlayer water bath to make the block The methyl-ortho-vanillin is completely dissolved, and the stirring is stopped. Intense foam is produced during the reaction, and the temperature continues to rise. At this time, water droplets can be seen in the cup. When there are no water droplets in the cup, it is the end of the reaction. Continue to keep warm 15 minutes, keep warm at 150°C, cool down to below 60°C, and pump into the autoclave;

[0043] S2: Hydrogenation reaction: pump the catalyst into the autoclave. After all the materials are added, the liquid level reaches the turbine position of the autoclave. After repeated ventilation with hydrogen for thre...

Embodiment 3

[0056] This kind of rotundine production technology comprises the steps:

[0057] S1: Manufacture of Schiff's base: Add piperethylamine measured by a balance scale into the condensation tank, add polyoxymethylene under stirring, open the vacuum system to make the vacuum in the tank reach 0.06MPa, and then slowly heat in the interlayer water bath to make the block The methyl-ortho-vanillin is completely dissolved, and the stirring is stopped. Intense foam is produced during the reaction, and the temperature continues to rise. At this time, water droplets can be seen in the cup. When there are no water droplets in the cup, it is the end of the reaction. Continue to keep warm 16 minutes, holding temperature 160°C, cooling down to below 60°C, pumping into the autoclave;

[0058] S2: Hydrogenation reaction: pump the catalyst into the autoclave. After all the materials are added, the liquid level reaches the turbine position of the autoclave. After repeated ventilation with hydrogen...

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Abstract

The invention discloses a production process of rotundine in the technical field of rotundine production. The production process of rotundine includes the following steps: manufacturing of Schiff base, hydrogenation reaction, concentration, neutralization and crystallization, centrifugal filtration, drying, cyclization reaction, copper removal reaction, reduction, splitting, refining, drying and total mixing and packaging. The production process of rotundine is reasonably designed; through multilayer complex process, side-effect products in the preparation process are filtered out step by stepto reduce the side-effects of the products while the original efficacy of the prepared product is ensured. By improvement of the proportion of the preparation raw materials, the efficacy time of theproduct is prolonged and the efficacy is maintained for a long time.

Description

technical field [0001] The invention relates to the technical field of rotundine production, in particular to a rotundine production process. Background technique [0002] Rotundine has analgesic, sedative, hypnotic and stable effects. Its analgesic effect is weaker than pethidine, stronger than general antipyretic analgesics. At therapeutic doses, it has no respiratory depressant effect and does not cause gastrointestinal smooth muscle spasm. It is better for chronic persistent pain and visceral dull pain, but less effective for acute sharp pain (such as postoperative pain, traumatic pain, etc.) and advanced cancer pain. While producing analgesic effect, can cause sedation and hypnosis, but present rotundine also has the following problems because of the deficiency of preparation technology: the rotundine product efficacy maintenance time of making is short, and side effect height is easy to patient's pain. Use causes secondary injury, for this reason, we propose a kind ...

Claims

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Application Information

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IPC IPC(8): C07D455/03
CPCC07D455/03
Inventor 王志良李勇义杨彦熙胡宇鲁烨曹唐
Owner 佑华制药(乐山)有限公司
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