376591-99-0Relevant articles and documents
Method for synthesizing eltrombopag by using micro-channel reactor
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Paragraph 0035; 0071-0085; 0088-0089, (2021/04/14)
The invention discloses a method for synthesizing eltrombopag by using a micro-channel reactor. The method comprises the following steps: S1, material synthesis: adding a raw material 3, 4-dimethylaniline into an acid aqueous solution, dissolving to obtain a material I, dissolving sodium nitrite into water to obtain a material II, dissolving sodium hydrogen sulfite and sodium hydroxide into water to obtain a material III, taking a solution prepared from hydrochloric acid and water as a material IV, adding a raw material 3-amino-2 hydroxyl-[1, 1-biphenyl]-3 formic acid into the acid aqueous solution, dissolving to obtain a material V, and dissolving sodium nitrite into water to obtain a material VI; s2, introducing the material into the micro-channel reactor S3 to obtain a first intermediate 3, 4-dimethylphenylhydrazine hydrochloride, and reacting with ethyl acetoacetate to obtain a second intermediate 2-(3, 4-dimethylphenyl)-5-methyl-1H-pyrazole-3 (2H)-ketone; and S4, introducing the material V and the material VI into the micro-channel reactor for reaction, and enabling the effluent reaction liquid to directly flow into a reaction bottle filled with a 2-(3, 4-dimethylphenyl)-5-methyl-1H-pyrazole-3 (2H)-ketone solution, thereby obtaining eltrombopag.
Continuous production process of eltrombopag
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Paragraph 0036; 0039; 0041; 0044; 0046; 0049; 0051; 0054;, (2020/08/27)
The invention discloses a continuous production process of eltrombopag. According to the method, a solid reaction container designed in combination with a 3D printing technology is adopted, all the steps in each corresponding reaction chambers are connected in series, raw materials are subjected to nitro reduction, hydrochloric acid acidification and diazotization in sequence and then subjected tocoupling, salifying and refining, and finally, automatic continuous synthesis of eltrombopag is achieved. According to the process, complex manual operation is not needed, chemical synthesis is rapidly carried out, the yield of a synthetic route is improved in a flowing chemical mode, and safety problems caused by manual operation is avoided. The design concept of the invention also reduces the loss of raw materials and solvents, realizes safe, efficient, economical and green continuous synthesis of the drug eltrombopag, and brings a brand-new mode and practical economic benefits to the preparation of the drug.
PROCESS FOR PREPARATION OF SUBSTITUTED 3'-HYDROAZINO-DIPHENYL-3-CARBOXYLIC ACID COMPOUNDS
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Paragraph 0220, (2015/03/31)
The present invention provides a process for the preparation of substituted 3′-hydrazino-biphenyl-3-carboxylic acid compounds. The present invention further provides a process for the preparation of 3′-{N′-[1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydr