Continuous synthesis for oseltamivir phosphate

A technology of oseltamivir phosphate and its synthesis method, which is applied in the field of continuous oseltamivir phosphate compound and its preparation, can solve the problems of cumbersome preparation steps, long production cycle and high cost, and achieve simple pipeline route and reduce time , the effect of small footprint

Active Publication Date: 2020-01-17
苏州奥普拓新材料有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method has a long preparation period and cumbersome preparation steps. In the laboratory test, solutions such as strong acid and strong alkali are used, and the safety requirements of the experiment are high, so it is not suitable for large-scale industrial production.
[0007] In order to improve the synthesis yield of oseltamivir phosphate, researchers have carried out a lot of research, but the preparation methods at home and abroad still have low yield, high cost, long production cycle, use of toxic and explosive products in the preparation process, and the heavy metal content of the product is not high. Problems such as reaching the standard, can't satisfy people's demand to the output of oseltamivir, therefore, need to provide a kind of production cost low, the preparation method of high output and yield urgently now

Method used

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  • Continuous synthesis for oseltamivir phosphate
  • Continuous synthesis for oseltamivir phosphate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] A synthetic method for continuous oseltamivir phosphate, comprising the following steps:

[0060] (1) Configuration solution: configure solution A and solution B respectively;

[0061] Solution A is a dehydrated ethanol solution of 35.52% by weight of intermediate 11 composed of 1074.00kg intermediate 11, 3023.65kg dehydrated alcohol and 0.20kg triphenylphosphine;

[0062] Solution B is the dehydrated ethanol solution of 1.3-dimethylbarbituric acid of 14.14% by weight of 427.54kg1.3-dimethylbarbituric acid, 3023.65kg dehydrated alcohol and 0.20kg triphenylphosphine composition ;

[0063] After adding solution A and solution B to the mixing module at the same time for mixing, mix to obtain mixture C; wherein the solution

[0064] A and solution B are transported by a metering diaphragm pump, and the transport flow rate is 0.99L / min;

[0065] (2) Reaction: transfer the mixture C to the reaction module, and the reaction module is loaded with a mesh-shaped high-performan...

Embodiment 2

[0074] A synthetic method for continuous oseltamivir phosphate, comprising the following steps:

[0075] (1) Configuration solution: configure solution A and solution B respectively;

[0076] Solution A is a dehydrated ethanol solution of 35.52% by weight of intermediate 11 composed of 1074.00kg intermediate 11, 3023.65kg dehydrated alcohol and 0.20kg triphenylphosphine;

[0077] Solution B is the dehydrated ethanol solution of 1.3-dimethylbarbituric acid of 14.14% by weight of 427.54kg1.3-dimethylbarbituric acid, 3023.65kg dehydrated alcohol and 0.20kg triphenylphosphine composition ;

[0078] After adding solution A and solution B to the mixing module at the same time for mixing, mix to obtain mixture C; wherein the solution

[0079] A and solution B are transported by a metering diaphragm pump, and the transport flow rate is 1.00L / min;

[0080] (2) Reaction: transfer the mixture C to the reaction module, and the reaction module is loaded with a mesh-shaped high-performan...

Embodiment 3

[0088] A synthetic method for continuous oseltamivir phosphate, comprising the following steps:

[0089] (1) Configuration solution: configure solution A and solution B respectively;

[0090] Solution A is a dehydrated ethanol solution of 35.52% by weight of intermediate 11 composed of 1074.00kg intermediate 11, 3023.65kg dehydrated alcohol and 0.20kg triphenylphosphine;

[0091] Solution B is the dehydrated ethanol solution of 1.3-dimethylbarbituric acid of 14.14% by weight of 427.54kg1.3-dimethylbarbituric acid, 3023.65kg dehydrated alcohol and 0.20kg triphenylphosphine composition ;

[0092] After adding solution A and solution B to the mixing module at the same time for mixing, mix to obtain mixture C; wherein the solution

[0093] A and solution B are transported by a metering diaphragm pump, and the transport flow rate is 1.01L / min;

[0094] (2) Reaction: transfer the mixture C to the reaction module, and the reaction module is loaded with a mesh-shaped high-performan...

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Abstract

The invention discloses a preparation method for an oseltamivir phosphate compound, and belongs to the field of organic chemistry. The method is a continuous and automated method for producing compounds. The preparation method includes the following processes: preparing a solution, performing a reaction, performing mixing, performing centrifuging, performing stirring, performing heating, performing decoloring, performing cooling, and performing centrifuging and drying. Reactants are conveyed by using a metering diaphragm pump, the output of a product is adjusted by adjusting the conveying speed, and the target product is finally obtained by centrifugal drying. The preparation method greatly shortens the production cycle, reduces the manual use, improves the safety in the production process, and reduces the use of materials.

Description

technical field [0001] The invention belongs to the field of organic chemistry, and in particular relates to a continuous oseltamivir phosphate compound and a preparation method thereof. Background technique [0002] Influenza is an acute respiratory infection caused by RNA (Ribonucleic Acid, ribonucleic acid) virus. There are many ways of its transmission, such as airborne transmission, human-to-human contact transmission or contact with contaminated objects for transmission, etc., and has a very high mortality rate in critically ill patients. Moreover, the mutation rate of influenza virus is extremely high and highly contagious, and genes are easy to reassort and mutate. Once influenza breaks out, it will cause huge death and property loss. It is known that 10%-20% of people in the United States are affected every year, and at least more than 10,000 people are killed each year, causing economic losses of up to 100 million U.S. dollars. [0003] After the influenza virus ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C231/00C07C231/12C07C233/52
CPCC07C231/12C07C231/00C07C2601/16C07C233/52
Inventor 陈晓高明军
Owner 苏州奥普拓新材料有限公司
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