- Method for synthesizing eltrombopag by using micro-channel reactor
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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.
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Paragraph 0035; 0052-0070; 0086-0087
(2021/04/14)
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- A 3 - methyl -1 - (3, 4 - dimethyl phenyl) -2 - pyrazoline -5 - one hydrochloride preparation method
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The present invention discloses a pharmaceutical intermediate 3 - methyl - 1 - (3, 4 - dimethyl-phenyl) - 2 - pyrazoline - 5 - one hydrochloride of a preparation method. The invention by improving the preparation method of the diazonium salt, the Na2SO3, replace the stannous chloride powder, reduces the use of toxic compounds, prepared by the method is a good drug for treating thrombocytopenia key intermediate, and simple preparation method of the present invention, the preparation conditions are not severe, has high commercial value.
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Paragraph 0020; 0028; 0029
(2019/03/31)
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- Synthesis of Aryl Hydrazines via CuI/BMPO Catalyzed Cross-Coupling of Aryl Halides with Hydrazine Hydrate in Water
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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.
- Kumar, Siripuram Vijay,Ma, Dawei
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supporting information
p. 1003 - 1006
(2018/09/20)
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- Double-ring substituted pyrazolone azo derivatives, their preparation and use (by machine translation)
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The invention belongs to the field of pharmaceutical chemicals, relates to a twin-ring substituted pyrazolone azo derivatives, preparation method thereof, its pharmaceutical composition and use thereof. In particular, the present invention is shown in formula I compound or its pharmaceutically acceptable salt or solvate. The invention relates also to the preparation method of the compound I, which comprises a pharmaceutical composition and their pharmaceutical use. The invention of the formula I compounds are effective TPO agonist, is good medicine for treating thrombocytopenia. Type I. (by machine translation)
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Paragraph 0095; 0105; 0106; 0107
(2017/01/02)
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- Facile and convenient synthesis of aryl hydrazines via copper-catalyzed C-N cross-coupling of aryl halides and hydrazine hydrate
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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.
- Kurandina, Daria V.,Eliseenkov, Eugene V.,Ilyin, Petr V.,Boyarskiy, Vadim P.
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p. 4043 - 4048
(2014/06/09)
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- Indole synthesis by rhodium(III)-catalyzed hydrazine-directed C-H activation: Redox-neutral and traceless by N-N bond cleavage
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Fishing for complements! There is an alternative to the useful Fischer indole synthesis. The new method utilizes the same retrosynthetic disconnection but is based on a RhIII-catalyzed directed C-H activation step and a successive coupling with alkynes. Copyright
- Zhao, Dongbing,Shi, Zhuangzhi,Glorius, Frank
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supporting information
p. 12426 - 12429
(2013/12/04)
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