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A kind of production technology of levodropropizine

A levodropropizine and production process technology, which is applied in the field of levodropropizine production process, can solve the problems of increased risk factor, large solvent odor, high price, etc., and achieve reduction of raw material costs, environmental protection pressure, Produce less dangerous effects

Active Publication Date: 2018-01-26
山东诚汇双达药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In this synthesis process, although the product with higher liquid phase purity is obtained, alcohols are used as the reaction medium, and the price is relatively expensive.
In addition, strong base catalysts such as sodium hydroxide are added as solids in this patent, and the alkalinity is too strong to be suitable for reaction, resulting in low yield
In addition, the salt produced in the reaction in this patent is removed through thermal filtration and crystallized again. Thermal filtration itself is not easy to operate, so the method is cumbersome to operate and is not suitable for large-scale industrial production; The solvent has reached the boiling point and is more volatile, which is not conducive to solvent recovery and pollutes the environment. In addition, the volatilization of alcohol solvents will easily cause a strong smell of solvents in the workshop during filtration, and alcohol solvents are flammable, which increases the risk factor in the production process.

Method used

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  • A kind of production technology of levodropropizine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] 1. Prepare 20% sodium hydroxide aqueous solution:

[0036] Pump 416 kilograms of deionized water into a 1000-liter reactor, add 104 kilograms of sodium hydroxide under stirring, and after dissolving, circulate water into the interlayer of the reactor and cool it down to room temperature for later use;

[0037] 2. Prepare the crude product of levodropropizine:

[0038] After checking that the 3,000-liter reactor is clean, 400 kg of N-phenylpiperazine (GC: 95%), 288 kg of R-(-)-3-chloro-1,2-propanediol, and 1,280 kg of deionized water were poured in sequence. Put it into the reaction kettle, pour in brine to cool down to 16°C, start adding 20% ​​lye dropwise, the temperature is still controlled at 15-30°C, pay close attention to and control the pH=8-12 during the dropwise addition, and the dropwise addition is completed in 1.5 hours. After the dropwise addition, close the brine valve, keep stirring at 20°C for 30 minutes, then raise the temperature to 42°C and keep it wa...

Embodiment 2

[0042] 1. Prepare 20% sodium hydroxide aqueous solution:

[0043] Pump 416 kilograms of deionized water into a 1000-liter reactor, add 104 kilograms of sodium hydroxide under stirring, and after dissolving, circulate water into the interlayer of the reactor and cool it down to room temperature for later use;

[0044] 2. Prepare the crude product of levodropropizine:

[0045] After checking that the 3,000-liter reactor is clean, 400 kg of N-phenylpiperazine (GC: 95%), 288 kg of R-(-)-3-chloro-1,2-propanediol, and 1,280 kg of deionized water were poured in sequence. Put it into the reaction kettle, pour in salt water to cool down to 18°C, start to add 20% lye dropwise, the temperature is still controlled at 15-30°C, pay close attention to and control the pH=9-11 during the dropwise addition, and the dropwise addition is completed in about 1 hour and 20 minutes . After the dropwise addition, close the brine valve, continue to insulate and stir at 22°C for 30 minutes, then raise...

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Abstract

The invention belongs to the technical field of chemical synthesis and in particular relates to a production process of levodropropizine. The production process of levodropropizine comprises the following steps: with water as a medium, reacting N-phenylpiperazine and R-(-)-3-chloro-1,2-propanediol in the presence of a catalyst sodium hydroxide to obtain a crude product of levodropropizine, thereby obtaining a refined product of levodropropizine after refining the crude product. The production process has the advantages of low production cost, high yield, high product quality and environment friendliness.

Description

technical field [0001] The invention belongs to the technical field of chemical synthesis, and in particular relates to a production process of levodropropizine. Background technique [0002] Levodropropizine chemical name (S)-3-(4-phenyl-1-piperazinyl)-1,2-propanediol, its molecular formula is C 13 h 20 N 2 o 2 . Levodropropizine is a chiral antitussive and expectorant drug developed and listed by Italian Dompe' Farm S.P.A in 1988. Hydroxyphenylpiperazine is the same, but the side effects are significantly reduced, and there is almost no central sedative effect of Hydroxyphenylpiperazine. The site of action is the site related to the sensory neuropeptide behind the peripheral node, and has a strong antitussive effect with a long duration; it is suitable for dry cough and persistent cough caused by acute upper respiratory tract infection and acute bronchitis. [0003] At present, there are mainly two methods for synthesizing levodropropizine: one is an asymmetric synth...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D295/088
CPCC07B2200/07C07D295/088
Inventor 曹晓华杨彦军王永广刘学文庞怀雷李跃东
Owner 山东诚汇双达药业有限公司