- Synthesis method of bixafen
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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.
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Paragraph 0023; 0025; 0028; 0030; 0033-
(2019/10/01)
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- Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains
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The spread of infections caused by multidrug-resistant (MDR) pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant S. aureus (VRSA), has created a need for new antibiotics with novel mechanisms of action. The bacterial division protein FtsZ has been identified as a novel drug target that can be exploited clinically. As part of an ongoing effort to develop FtsZ-targeting antibacterial agents, we describe herein the design, synthesis and bioactivity of six series of novel 1,3,4-oxadiazol-2-one-containing, 1,2,4-triazol-3-one-containing and pyrazolin-5-one-containing benzamide derivatives. Among them, compound A14 was found to be the most potent antibacterial agent, much better than clinical drugs such as ciprofloxacin, linezolid and erythromycin against all the tested gram-positive strains, particularly methicillin-resistant, penicillin-resistant and clinical isolated S. aureus. Subsequent studies on biological activities and docking analyses proved that A14 functioned as an effective compound targeting FtsZ. Preliminary SAR indicated a general direction for further optimization of these novel analogues. Taken together, this research provides a promising chemotype for developing newer FtsZ-targeting bactericidal agents.
- Bi, Fangchao,Song, Di,Qin, Yinhui,Liu, Xingbang,Teng, Yuetai,Zhang, Na,Zhang, Panpan,Zhang, Nan,Ma, Shutao
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p. 3179 - 3193
(2019/06/17)
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- Preparation method of Eltrombopag
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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.
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Paragraph 0013; 0014
(2018/04/28)
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- Oxidative radical arylation of anilines with arylhydrazines and dioxygen from air
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Substituted 2-aminobiphenyls have been prepared from arylhydrazine hydrochlorides and anilines in biphasic radical arylation reactions with dioxygen from air as a most simple and readily available oxidant. Under optimized conditions, the free amino functionality of the aniline leads to high ortho:meta regioselectivities, now even for anilines bearing a donor substituent in the para position. Finally, the mild and metal-free new access to aminobiphenyls was shown to be applicable on a gram scale.
- Hofmann, Josefa,Jasch, Hannelore,Heinrich, Markus R.
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p. 2314 - 2320
(2014/04/03)
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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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