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Synthesis method of sulfadiazine

A technology of sulfadiazine and its synthesis method, which is applied in the field of synthesis of sulfadiazine, and can solve the problems of high pressure on environmental protection, pollution, and high price

Pending Publication Date: 2021-03-12
CHONGQING KANGLE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Using diethylaminoacrolein as a raw material, a large amount of dimethylamine gas is produced after the reaction is completed, which seriously pollutes the atmosphere. Using vinyl ether and phosphorus oxychloride to synthesize a three-carbon compound, in addition to producing a large amount of dimethylamine gas, the reaction will also produce A large amount of phosphorus-containing wastewater, the pressure on environmental protection is very high
CN 105254575 discloses a new synthetic route, which uses malondialdehyde and sulfamidine as raw materials for synthesis; malondialdehyde raw materials are not easy to obtain, the price is high, and it is not suitable for industrial production

Method used

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  • Synthesis method of sulfadiazine
  • Synthesis method of sulfadiazine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Add 800g of toluene, 233.7g (1mol) of p-acetamidobenzenesulfonyl chloride, and 95.1 (1mol) g of 2-aminopyrimidine into a 2L reaction flask, stir at 20°C to 30°C, add 200g (2mol) of powdered calcium carbonate, and heat up to 55 ℃ ~ 65 ℃ heat preservation reaction, after the reaction is completed, add 300g of 20% sodium hydroxide aqueous solution, heat up to 100 ℃ ~ 115 ℃ for reaction, after the reaction is completed, cool down, let it stand, the upper layer of toluene layer is used mechanically, and the lower layer of water layer is slowly dripped with concentrated hydrochloric acid, Adjust the pH of the system to 5.0-5.5, filter, wash the filter cake with a large amount of water, and dry to obtain sulfadiazine with a yield of 98.2%.

Embodiment 2

[0020] Add 800g of toluene, 233.7g (1mol) of p-acetamidobenzenesulfonyl chloride, 95.1g (1mol) of 2-aminopyrimidine into a 2L reaction flask, stir at 20°C to 30°C, add 100g (1mol) of powdered calcium carbonate, and heat up to 55 ℃ ~ 65 ℃ heat preservation reaction, after the reaction is completed, add 300g of 20% sodium hydroxide aqueous solution, raise the temperature to 100 ℃ ~ 115 ℃ for reaction, after the reaction is completed, cool down, let it stand, apply the upper layer of toluene, and slowly add concentrated hydrochloric acid dropwise to the lower layer to adjust the system pH 5.0-5.5, filter, wash the filter cake with a large amount of water, and dry to obtain sulfadiazine with a yield of 87.4%.

Embodiment 3

[0022] Add 800g of toluene, 233.7g (1mol) of p-acetamidobenzenesulfonyl chloride, and 95.1g (1mol) of 2-aminopyrimidine in a 2L reaction flask, stir at 20°C to 30°C, add 150g (1.5mol) of powdered calcium carbonate, and heat up to 55 ℃ ~ 65 ℃ heat preservation reaction, after the reaction is completed, add 300g of 20% sodium hydroxide aqueous solution, heat up to 100 ℃ ~ 115 ℃ for reaction, after the reaction is completed, cool down and let it stand, the upper layer of toluene layer is used mechanically, and the lower layer of water layer is slowly dripped with concentrated hydrochloric acid, Adjust the pH of the system to 5.0-5.5, filter, wash the filter cake with a large amount of water, and dry to obtain sulfadiazine with a yield of 96.0%.

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Abstract

The invention discloses a synthesis method of sulfadiazine. The method is characterized in that 4-acetamidobenzenesulfonyl chloride and 2-aminopyrimidine are used as initial raw materials, powdered calcium carbonate is used as an acid-binding agent for condensation, and then hydrolysis and acidification are carried out to synthesize sulfadiazine. According to the invention, the defects that at present, anhydrous pyridine and other organic bases are adopted as acid-binding agents, wherein pyridine can seriously pollute the environment, is difficult to recover and causes great safety threats tothe body health of workers are overcome, and the method is easy and convenient to operate, environmentally friendly and suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical fields of medicine and chemical industry, and in particular relates to a synthesis method of sulfadiazine. Background technique [0002] Sulfadiazine (Sulfadiazine) is a sulfonamide anti-infective drug commonly used clinically in my country at present, also known as sulfapyridazine and diyajing. Sulfadiazine is effective against hemolytic streptococcus, staphylococcus, meningococcus, pneumococcus, Neisseria gonorrhoeae, Escherichia coli, Shigella and other sensitive bacteria, as well as Chlamydia trachomatis, actinomycetes, Plasmodium, Nocardia astrocytes and Toxoplasma gondii, etc. Microorganisms are inhibited. The advantages of sulfadiazine are high effective concentration in blood, low serum protein binding rate, and easy penetration of the drug into cerebrospinal fluid. It is the drug of choice for the treatment of epidemic meningitis. [0003] CN 105254575 mentions two main synthetic routes, one is to use p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/69
CPCC07D239/69
Inventor 杨忠鑫刘震洋宋小莉谢晓芹蔡中文杨继斌
Owner CHONGQING KANGLE PHARMA
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