- Preparation method of triazinone ring
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A preparation method of a triazinone ring relates to the technical field of veterinary drugs, and comprises the following steps: carrying out a diazo condensation reaction on a condensation compound aniline and potassium ethyl malonate, carrying out an amidation reaction with sodium cyanate under an acidic condition, adding acetic acid and sodium acetate, heating, heating, and carrying out a cyclization reaction to obtain a triazinone compound. According to the method, operations such as filtration and separation are not needed before the finished product is obtained, the product loss is reduced, the method has the advantages of simple process and high yield, the yield of the salmizuril can reach 89.65%-94.81%, and the yield of the diclazuril can reach 80.20%-94.11%; and the problem of odor generation of decarboxylation reaction in the production process is also solved, and the method is beneficial to environmental protection and suitable for industrial production.
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Paragraph 0038-0051
(2021/08/14)
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- Method for preparing 2-[phenyl]-1, 2, 4-triazine-3, 5 (2H, 4H)-dione compound
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The invention relates to the technical field of veterinary drugs, in particular to a method for preparing a 2-[phenyl]-1, 2, 4-triazine-3, 5 (2H, 4H)-dione compound. The method comprises the following steps: (1) taking dichloroacetyl chloride and ethyl carbamate as reaction raw materials, adding an acid-binding agent and a reaction solvent, heating, and carrying out heat preservation reaction, distillation and rectification treatment to obtain (2, 2-dichloroacetyl) ethyl carbamate; (2) adding the aniline compound as shown in the structural formula II into hydrochloric acid, treating with a diazotization reagent, a reduction reagent and an acidification reagent, and neutralizing and washing with water to obtain the phenylhydrazine compound as shown in the structural formula III; and (3) adding a phenylhydrazine compound and (2, 2-dichloroacetyl) ethyl carbamate into anhydrous acetic acid, adding a reaction aid, heating until the reaction is finished, and then carrying out distillation treatment to obtain the 2-[phenyl]-1, 2, 4-triazine-3, 5 (2H, 4H)-dione compound. By utilizing the method, the whole reaction steps are shortened, the economic benefit is improved, and the emission of three wastes is reduced.
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Paragraph 0024-0027
(2021/08/14)
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- A coccidian preparation method
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The invention relates to a preparation method for diclazuril. A document reports that the synthesis of diclazuril is carried out in a such way that 2,6-dichloro-para-nitroaniline or 3,4,5-trichloronitrobenzene is used as an initial raw material and is subjected to diazotization reaction, substitution reaction, reduction reaction and the like to prepare a common intermediate 3. The existing process has many steps and is low in overall yield so that the costs of diclazuril raw materials and preparation stay at a high level. The invention provides a synthetic process of diclazuril. Particularly, the synthetic process comprises the steps that an intermediate 4 is prepared by performing reaction on the intermediate 3 and sodium nitrite by means of reduction and is subjected to cyclization and ring enlargement to obtain a product. In the route, a column chromatography means is not adopted; therefore, the process is short in the reaction steps and is suitable for industrial production.
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- Diclazuril and isotope internal standard D4-Diclazuril method for the preparation of
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The invention relates to a preparation method for diclazuril and isotope interior label D4-diclazuril. In the invention, 2, 6-dichloro-4-nitroaniline is adopted as a raw material, and the raw material is subjected to a sandmeyer reaction, affinity substitution, reduction, diazotization, diazonium reduction, a two-step condensation reaction, cyclization and refining, so that the diclazuril or the isotope interior label D4-diclazuril competitive product is obtained. According to the invention, during the process, the affinity substitution and the nitro-reduction can be continuously implemented without processing, and the diazotization, the diazonium reduction as well as the two-step condensation reaction can realize one-pot synthesis, the material prepared is high in purity and can reach 99.5%, the total yield is increased by about 10% as compared with that of the prior art, and the blank of the detection field of the medicine is filled up.
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- 1, 2, 4-Triazin-3-one derivatives, production and use thereof
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The present invention provides a novel triazine derivative of the formula STR1 wherein ring A is an optionally substituted aromatic group; X is an oxygen or sulfur atom; R1 and R6 are each a hydrogen atom or an optionally substituted hydrocarbon residue or heterocyclic group which may bound through a hetero-atom; R2 and R3 are each independently a hydrogen atom, a halogen atom, or a group bound through a carbon, oxygen or sulfur atom, or taken together, represent =S; R4 and R5 are each independently a hydrogen atom, a halogen-atom, or a group bound through a carbon, oxygen, nitrogen or sulfur atom; R1 and R2, and R5 and R6 may each bind together to form a chemical bond; provided that where ring A is a phenyl group having at least a halogen atom in position -2 or 4 and X is an oxygen atom, R4 and R5 do not conjoin to form a chemical bond, or a salt thereof. The invention also encompasses an antiprotozoan composition comprising the novel triazine derivative or a salt thereof.
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- Anti-protozoal α-aryl-4-(4,5-dihydro-3,5-dioxo-1,2,4-triazin-2(3H)-yl)-benzeneacetonitrile derivatives, pharmaceutical compositions, and method of use therefor
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The present invention is related with α-aryl-4-(4,5-dihydro-3,5-dioxo-1,2,4-triazin-2(3H)-yl)benzeneacetonitriles which are effective in destructing or preventing the growth of Protozoa in subjects suffering from such Protozoa.
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