19763-90-7Relevant articles and documents
Synthesis method of bixafen
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Paragraph 0023; 0025; 0028; 0030; 0033-, (2019/10/01)
The invention relates to a synthesis method of bixafen. The method comprises the steps that firstly, 3,4-dichloroaniline is prepared into 3,4-dichloro phenylhydrazine hydrochloride through a reductionagent, then air is introduced into the 3,4-dichloro phenylhydrazine hydrochloride under an alkaline environment, the 3,4-dichloro phenylhydrazine hydrochloride and para-fluoroaniline are subjected tooxidative coupling for obtaining an intermediate 3',4'-dichloro-5-fluorine-2-benzidine, and finally the intermediate and 1-methyl-3-difluoro methyl-4-parazole formyl chloride are subjected to an amidation reaction for preparing the bixafen. According to the adopted technology, the reaction conditions are mild and easy to control, operation is easily and conveniently conducted, the product is easyto purify, and the product can be obtained directly through recrystallization. The control method for intermediates in all steps is simple and accurate, the product yield is high, the atom economy isgood, complex aftertreatment of an old method is avoided, and the method has great competitive advantages and high industry production utilization value. Meanwhile, application of raw materials, withhigh dangerousness, such as butyllithium is avoided, generation of a large amount of solid waste of tarry substances is avoided, the content of the three wastes is extremely low, and the method accords with the concept of environment-friendly chemistry.
Preparation method of Eltrombopag
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Paragraph 0013; 0014, (2018/04/28)
The invention discloses a preparation method of Eltrombopag. The chemical name of Eltrombopag is 3-{(2Z)-2-[1-(3,4-xylyl)-3-methyl-5-oxo-1,5-dihydro-4H-parazole-4-ylidene]diazanyl}-2-hydroxy-3-biphenylcarboxylic acid-2-aminoethanol salt. The process of the preparation technique of the preparation method of Eltrombopag is simple, materials are easy to obtain, and the preparation method of Eltrombopag is cost-efficient and environment-friendly, can help realize industrialization, can promote the economic and technological development of the Eltrombopag active pharmaceutical ingredient, reduce the production cost, and is suitable for mass production.
Indole synthesis by rhodium(III)-catalyzed hydrazine-directed C-H activation: Redox-neutral and traceless by N-N bond cleavage
Zhao, Dongbing,Shi, Zhuangzhi,Glorius, Frank
supporting information, p. 12426 - 12429 (2013/12/04)
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