Antibiotic Raw Materials Oxolinic Acid Powder

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Oxolinic Acid Powder Usage and Synthesis.

Oxyquinic acid, also known as oxcyclic oxoquinic acid, oryzolinic acid, oryzolinic acid, belongs to the second generation of quinolone fungicide, white with yellowish-white columnar crystals or crystalline powder at room temperature, odourless, tasteless, with strong antibacterial efficacy against Gram-negative bacteria and a part of the positive bacteria, and no cross-resistance with antibiotics, but there is no antibacterial effect on the fungi and Mycobacterium tuberculosis, has the advantages of low dosage, good bacteriostatic effect and so on.

Mainly used in the treatment of fish, shrimp bacterial diseases, aquaculturists believe that it is one of the more ideal drugs for the treatment of aquatic animal diseases, Vibrio eel, Aeromonas hydrophila and other fish pathogens have a fairly strong antibacterial activity.

Therefore, it is widely used in Japan, Taiwan Province of eel and other aquatic animals, in sea water aquaculture PH has a slight effect on it, in the alkaline environment need to increase the dosage of the drug.

The toxicity of oxalic acid is very little, acute, toxicity test on carp oral LD50 (i.e., under the influence of a certain concentration of the drug can make 50% of the time of individual death) for more than 4000mg/kg.

The use of the drug must be stopped 25 days before use, otherwise the residue exceeds the standard, the Japanese market banned imports, Taiwan updated Oxolinic acid (Oxolinicacid) in fish, shrimp, eggs, cattle, pigs, chickens, muscle, fat, liver and kidney, such as thirteen residue tolerance.

Uses and functions of Oxolinic Acid.

Quinolone fungicide, used for rice seed treatment, is known as the first fungicide with high efficacy against the hard-to-treat disease of rice, bacterial blight (seedling rot).

Seed dressing treatment before sowing can inhibit the occurrence of Botrytis cinerea, and then prevent the occurrence of Botrytis cinerea after transplanting robust seedlings into the field.

The mechanism of action is a wide range of antibacterial activity against Gram-negative bacteria, but weak activity against Gram-positive bacteria and no activity against fungi. By inhibiting DNA synthesis, it hinders the division and proliferation of germs.

In the bacterial body, for the supercoiled structure of DNA imported reverse supercoiled enzyme, this agent can be combined with the subgroup A of this enzyme, so that its function is suppressed and the DNA can not be replicated, and soon cause death. It can be used to soak the seed at 1000g/mL for 24h, 1000g/mL for 10min, or 20% wettable powder to coat the seed at 0.5% of seed mass, and the preventive effect is more than 97%.

This product can also be used for the prevention and control of rice grain rot, potato black cavity disease, soft rot, fire blight and similar diseases.

For example, it can prevent rice grain rot by foliar spraying with 300-600g active ingredient/hm2 during the period of rice spiking; it can prevent fire blight and soft rot of apple and pear by foliar spraying with 300-600g active ingredient/hm2. It also has good protective and therapeutic effects on cabbage soft rot.

Has a strong broad-spectrum, Gram-negative bacteria and a portion of the positive bacteria have a strong antibacterial effect, and antibiotics without cross-pharmacy, but no antibacterial effect on fungi and tuberculosis mycobacteria, with a low dosage, good inhibition of bacterial effect and other advantages, aquaculturists believe that he is the treatment of aquatic animal diseases is one of the more desirable drugs.

Vibrio eel, Aeromonas hydrophila and other fish pathogens have considerable antibacterial activity.

Characteristic of Oxolinic Acid.

It is solid. m.p. 310°C, relative density 1.55(25°C), vapour pressure <1.46×10-4Pa(100°C). solubility <1.0% in acetone, ethyl acetate, methanol at 25°C, solubility 0.003mg/L in water.

Can act with sodium hydroxide to form salt, and its salt is soluble in water. Stable to heat, moisture and light.

Production Methods of  Bulk Oxolinic Acid Powder.

Preparation of methylenedioxyaniline was prepared by nitration and reduction of methylenedioxybenzene to methylenedioxyaniline.

Synthesis of quinuclidinone Methylenedioxyaniline and diethyl ethoxymethylmalonate were heated and reacted at 80-90°C for 3h, and then refluxed and cyclised in xylene, followed by N-alkylation with ethyl iodide in DMF solvent in the presence of sodium hydroxide at 70-75°C, and the mixture was diluted with water and then refluxed for 3-4h, and hydrolysed products were acidified with hydrochloric acid to produce quinuclidinone.

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