6975-73-1Relevant articles and documents
Intermediate for topipitastat, preparation method thereof, and method for preparing topipitastat from intermediate
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Paragraph 0035; 0044; 0045; 0046, (2018/07/30)
The invention belongs to the technical field of medicines, and particularly relates to an intermediate for topipitastat, a preparation method thereof, and a method for preparing topipitastat from theintermediate. The intermediate for the topipitastat is 3-(4-pyridyl)-5-(1-oxo-4-pyridyl)-1,2,4-triazole p-toluenesulfonate, and the structural formula of the intermediate is represented by formula (I). The preparation methods are characterized in that methyl isonicotinate oxynitride and hydrazine hydrate undergo a condensation reaction, a ring closing reaction and a salt formation reaction to obtain the intermediate, and the intermediate and N,N-dimethylformyl chloride undergo a cyanation reaction and a refining reaction to obtain the topipitastat. The methods effectively solve the technical problems of complex preparation process and low purity of topiroxostat, and have the advantages of simple process, good reproducibility, low cost, environmental protection and energy saving, so the methods have high industrial values and remarkable social and economic benefits. The preparation methods are used for preparing the key intermediate for the topiroxostat and the topiroxostat.
A method for synthesizing holds the pyrrole department he (by machine translation)
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Paragraph 0023; 0027; 0028, (2016/10/08)
The present invention provides a method for the synthesis of I he holds the pyrrole department, comprising the following steps: 1), II to isonicotinic acid methyl ester as the raw material, the presence of the oxidizing agent, is generated by the oxidation of isonicotinic acid methyl ester N-oxide III; 2), then condensation with hydrazine hydrate to obtain retozide N-oxide IV; 3), compound IV with 4-cyanopyridine mellow alkali V under the conditions of the reaction to produce 4 - (2 - (imino (pyridin-4-yl) methyl) [...] ) pyridine N-oxide VI; 4), the presence of the dimethyl carbamic chloride, and cyanide reaction to produce 2-cyano-Nˊ - (imino (pyridin-4-yl) methyl) retozide VII; 5), the resulting compound in the presence of an acid VII to cyclization, I have he holds the pyrrole department ; the reaction route is as follows: In the method of the invention, the total yield, on the one hand relative to the literature yield greatly improved, on the other hand, line is simple and easy to obtain the raw materials and low cost, the steps of the mild reaction conditions, the post-processing is simple; it is very easy to be industrialized control. (by machine translation)
