54826-14-1Relevant articles and documents
Synthesis method for aromatic ring bromination of acetophenones derivative
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Paragraph 0071-0074, (2019/06/11)
The invention relates to a synthesis method for aromatic ring bromination of an acetophenones derivative, and belongs to the technical field of organic synthesis. The synthesis method consists of twokinds of synthesis methods: method A, adding the acetophenone derivative into a first oxidizing agent and stirring to form a suspension system, controlling the temperature of the suspension system tobe 10-50 DEG C, adding a first reducing agent or a second reducing agent, stirring and reacting for 2-20 h, and performing aftertreatment after the reaction is completed to obtain the aromatic ring brominated acetophenone derivative; method B, adding the acetophenone derivative into the second reducing agent and stirring to form a suspension system, controlling the temperature of the suspension system to be 10-50 DEG C, then adding a second oxidizing agent or the first oxidizing agent, stirring and reacting for 2-20 h, and performing aftertreatment after the reaction is completed to obtain thearomatic ring brominated acetophenone derivative. According to the synthesis method provided by the invention, an inorganic and non-toxic bromination reagent is used, water is used as a reaction solvent, the prepared product is mutually incompatible with water, so that separation and the aftertreatment are convenient to perform, therefore, the synthesis method of the invention is applicable to large-scale industrial production of intermediate products for aromatic ring bromination of the acetophenones derivative.
Isoquinolinium Dichromate and Chlorochromate as Efficient Catalysts for Oxidative Halogenation of Aromatic Compounds under Acid-Free Conditions
Rao, A. Sambashiva,Rajanna,Reddy, K. Rajendar,Kulkarni, Subhash
, p. 832 - 837 (2016/02/12)
Isoquinolinium dichromate and isoquinolinium chlorochromate were found as efficient catalysts to trigger oxidative bromination and iodination of aromatic hydrocarbons with KBr/KI and KHSO4 under acid-free conditions. Reaction times reduced highly significantly under sonication, followed by corresponding mono bromo derivatives in very good yield with high regioselectivity.
Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors
Ameriks, Michael K.,Bembenek, Scott D.,Burdett, Matthew T.,Choong, Ingrid C.,Edwards, James P.,Gebauer, Damara,Gu, Yin,Karlsson, Lars,Purkey, Hans E.,Staker, Bart L.,Sun, Siquan,Thurmond, Robin L.,Zhu, Jian
scheme or table, p. 4060 - 4064 (2010/08/07)
A pyridazin-4-one fragment 4 (hCatS IC50 = 170 μM) discovered through Tethering was modeled into cathepsin S and predicted to overlap in S2 with the tetrahydropyridinepyrazole core of a previously disclosed series of CatS inhibitors. This fragment served as a template to design pyridazin-3-one 12 (hCatS IC50 = 430 nM), which also incorporates P3 and P5 binding elements. A crystal structure of 12 bound to Cys25Ser CatS led to the synthesis of the potent diazinone isomers 22 (hCatS IC50 = 60 nM) and 27 (hCatS IC50 = 40 nM).