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Synthesis method of sulfachloropyrazine sodium

A technology of sulfachlorpyrazine sodium and sulfachlorpyrazine sodium, which is applied in the field of synthesis of sulfachlorpyrazine sodium, can solve problems such as difficult removal and unsatisfactory, and achieve low price, high yield and product purity, and abundant sources of raw materials Effect

Active Publication Date: 2020-06-02
湖南吴赣药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The impurity is a by-product of condensation reaction, with a content of about 0.6%. The usual "acid and alkali method" refining is not easy to remove, and cannot meet the latest version of the European Pharmacopoeia.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0020] A kind of synthetic method of sulfachlorpyrazine sodium, is characterized in that, comprises the steps:

[0021] Step S1, sequentially add 4-aminobenzene-1-sulfonyl chloride, 2-amino-6-chloropyrazine and an organic solvent into the reaction kettle, and then slowly add an acid-binding agent therein, and complete the addition within 2-4 hours. Stir at 0.8-1.3MPa, 30-50°C for 12-20 hours to obtain the first mixed solution, and adjust the reaction kettle to normal temperature and pressure;

[0022] Step S2, removing the solvent by suction filtration of the first mixed solution prepared in step S1 to obtain a crude product, then adding drinking water to the crude product, adjusting the pH value to 4.5-5.3 with hydrochloric acid, filtering and washing with water to obtain sulfachlorpyr Zinc;

[0023] Step S3, heating and dissolving the sulfachlorpyrazine produced in step S2 in sodium hydroxide solution, cooling and crystallizing, and filtering to obtain sulfachlorpyrazine so...

Embodiment 1

[0034] Embodiment 1 provides a kind of synthetic method of sulfachlorpyrazine sodium, is characterized in that, comprises the steps:

[0035] Step S1, add 4-aminobenzene-1-sulfonyl chloride, 2-amino-6-chloropyrazine and toluene to the reaction kettle in turn, and then slowly add sodium hydroxide to it, within 2 hours, at 0.8MPa After stirring for 12 hours at 30°C, the first mixed solution was obtained, and the reaction kettle was adjusted to normal temperature and pressure;

[0036] Step S2, suction-filtering the first mixed solution prepared through step S1 to remove the solvent to obtain a crude product, then adding drinking water to the crude product, adjusting the pH value to 4.5 with hydrochloric acid, filtering and washing with water to obtain sulfachlorpyrazine;

[0037] Step S3, heating and dissolving the sulfachlorpyrazine produced in step S2 in sodium hydroxide solution, cooling and crystallizing, and filtering to obtain sulfachlorpyrazine sodium.

[0038] The molar...

Embodiment 2

[0042] Embodiment 2 provides a synthetic method of sulfachlorpyrazine sodium, which is basically the same as in Example 1, except that 4-aminobenzene-1-sulfonyl chloride, 2-amino-6-chloropyrizine described in step S1 The mol ratio of oxazine, organic solvent, acid-binding agent is 1:1:7:0.9; Described acid-binding agent is sodium carbonate.

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PUM

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Abstract

The invention relates to a synthesis method of sulfachloropyrazine sodium. The preparation method is characterized by comprising the following steps of: S1, sequentially adding 4-aminobenzene-1-sulfonyl chloride, 2-amino-6-chloropyrazine and an organic solvent into a reaction kettle, then slowly adding an acid-binding agent into the reaction kettle within 2-4h, and performing stirring for 12-20h under a pressure of 0.8-1.3MPa and a temperature of 30-50DEG C to obtain a first mixed solution; adjusting the pH value to 4.5-5.3 with hydrochloric acid, and performing filtering and washing to obtainsulfachloropyrazine; and S3, putting the sulfachloropyrazine prepared in S2 into a sodium hydroxide solution, performing heating for dissolving, conducting cooling for crystallization, and performingfiltering to obtain sulfachloropyrazine sodium. The synthesis method of sulfachloropyrazine sodium disclosed by the invention is simple and practicable, the raw material sources are rich, the price is low, the preparation efficiency, yield and product purity are high, the preparation process is green and environment-friendly, and good combination of economic benefits, social benefits and ecological benefits is effectively realized.

Description

technical field [0001] The invention relates to the technical field of chemical synthesis, in particular to a synthetic method of sulfachlorpyrazine sodium. Background technique [0002] Sulfachlorpyrazine sodium is also known as three-character coccidian powder, chemical name: 4-amino-N-(6-chloro-2-pyrazinyl)benzenesulfonamide sodium monohydrate, white or light yellow powder. It is an anti-inflammatory and antibacterial drug for poultry and livestock. It has the characteristics of fast absorption in animals, high bioavailability and tissue drug concentration, wide distribution in the body, strong antibacterial effect, long maintenance time, and does not affect the host's immunity to coccidia. It is mainly used to treat chicken, rabbit, sheep coccidiosis (cecal coccidiosis), chicken cholera and typhoid fever, and also has strong antibacterial effect, and has strong antibacterial activity against Pasteurella, Salmonella, etc., especially suitable for Prevention and control o...

Claims

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Application Information

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IPC IPC(8): C07D241/22
CPCC07D241/22
Inventor 钱炜雯韩菊泉刘永超
Owner 湖南吴赣药业有限公司