60481-51-8Relevant articles and documents
Method for synthesizing eltrombopag by using micro-channel reactor
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Paragraph 0035; 0052-0070; 0086-0087, (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.
Synthesis of Aryl Hydrazines via CuI/BMPO Catalyzed Cross-Coupling of Aryl Halides with Hydrazine Hydrate in Water
Kumar, Siripuram Vijay,Ma, Dawei
supporting information, p. 1003 - 1006 (2018/09/20)
The N,N’-bis(2,6-dimethylphenyl)oxalamide was discovered as a powerful ligand for Cu-catalyzed cross-coupling of aryl halides with hydrazine hydrate, leading to the formation of a variety of aryl hydrazines at 80 oC in water under the assistance of K3PO4 and 4 mol% cetyltrimethylammonium bromide from aryl bromides and aryl iodides. Good to excellent yields were observed in most cases.
Facile and convenient synthesis of aryl hydrazines via copper-catalyzed C-N cross-coupling of aryl halides and hydrazine hydrate
Kurandina, Daria V.,Eliseenkov, Eugene V.,Ilyin, Petr V.,Boyarskiy, Vadim P.
, p. 4043 - 4048 (2014/06/09)
An efficient and convenient method for the synthesis of aryl hydrazines has been developed via copper-catalyzed cross-coupling of aryl bromides and hydrazine with a readily accessible ligand and water as a solvent. The multigram scale procedure is applicable to aryl bromides bearing both moderately electron-donating and electron-withdrawing substituents in the aromatic nucleus. No column chromatography is required to obtain aryl hydrazine hydrochlorides in good yields.