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Diclazuril is a triazine benzeneacetonitrile compound, which is a new type of high efficiency (only 1g of this compound per tonne of feed), low toxicity (no toxicity was found in 50 times of overdose) anticoccidial drug, widely used in chickens for coccidiosis. In addition, it has preventive and therapeutic effects on many kinds of coccidia, and can also be used to prevent ducks, quails, turkeys, geese and rabbits from getting coccidiosis.
Diclazuril is a kind of new synthetic non-ion-carrying anticoccidial drug, the anticoccidial index of this product is above 180 for the six main types of Eimeria in chickens, which is a highly efficient anticoccidial drug, and it also has the features of low toxicity, broad-spectrum, small dosage, wide range of safety, no stopping period, no toxic side-effects, no cross-resistance, and it is not affected by the process of feed pelleting, etc.
Uses and functions of Diclazuril.
Anti-coccidiostat. It has a preventive effect on many kinds of coccidia and is used to prevent coccidiosis in chickens, ducks, quails, turkeys, geese and rabbits.
Countermeasures to prevent the emergence of drug resistance: Since resistance will emerge from the long-term use of an anti-coccidiostat, in order to avoid the emergence of drug resistance, shuttle drug use and rotational drug use can be used in the prevention programme.
In order to avoid the development of resistance, shuttle dosing and rotational dosing can be used in the prevention programme. In shuttle dosing, one type of anticoccidial is used at the beginning of the feeding cycle and another type of anticoccidial is used at the end of the cycle.
Rotational drug, in a year of rearing chickens, the first half of the year with an anticoccidial drug, the second half of the year with another anticoccidial drug application of the above two methods of drug use, so that the resistance to produce electricity or do not produce, to prolong the service life of anticoccidial drugs.
Pharmacological Effect of Diclazuril.
Diclazuril is a triazine benzeneacetonitrile compound, which is a new type of high efficient and low toxicity anticoccidial drug, widely used in chicken coccidiosis.
The mechanism of anti-coccidial action of diclazuril is not clear. The main action peak period of coccidia varies with different species of coccidia, such as the main action point of Eimeria flexneri in the sexual cycle of the 2nd generation of Schizothoracinum.
However, it is ineffective against Eimeria gigantica and Eimeria burgdorferi schizonts. The point of action for Eimeria megaterium is in the syncytial stage of the coccidia; for Eimeria burgdorferi, it is highly effective in the small gametophyte stage. Diclofenac also inhibits the formation of sporulated oocysts.
Production Method of Bulk Diclazuril Powder.
Hydrogen reduction of 2,6-dichloro-α-(4-chlorophenyl)-4-nitrobenzeneacetonitrile (A) to as 4-amino-2,6-dichloro-α-(4-chlorophenyl)benzeneacetonitrile (B) was carried out with hydrogen catalysed by 5% platinum-charcoal using methanol as a solvent.
(B) was diazotised and coupled to form ethyl 2-[[3,5-dichloro-4-[(4-chlorophenyl)cyanomethyl]phenyl]-hydrazinyl]-2-cyanoacetylcarbamate (C), (C) was cyclised and hydrolysed to form 2-[3,5-dichloro-4-[(4-chlorophenyl)cyanomethyl]phenyl]-2,3,4,5-tetrahydro-3,5-dicarbonyl-1,2,4-triazine -6-carboxylic acid (D). Using mercaptoacetic acid as a solvent, (D) undergoes a decarboxylation reaction at 170°C to produce diclazuril.
Among them, the cyclisation and hydrolysis were carried out as follows: 7.8 parts of compound (C), 1.98 parts of anhydrous potassium acetate and 120 parts of glacial acetic acid were stirred and refluxed for 3h, and after making up the appropriate amount of glacial acetic acid and 30 parts of concentrated hydrochloric acid, stirring and refluxing were continued for 10h; and then it was concentrated, cooled and filtered, and the filter cake was compound (D).
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