2924-09-6Relevant articles and documents
1,3-dibromo-4-fluorobenzene preparation method
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Paragraph 0011; 0014, (2019/02/27)
The invention discloses an industrial preparation method of 1,3-dibromo-4-fluorobenzene. The industrial preparation method of 1,3-dibromo-4-fluorobenzene comprises the steps that o-fluoronitrobenzeneserves as an initial raw material, and 1,3-dibromo-4-fluorobenzene is synthesized through bromine applying, reduction and diazotization-Sandmeyer three step reactions. The obtained 1,3-dibromo-4-fluorobenzene is yellow oily liquid, the purity is 97.5%, the raw material conversion rates of all steps each reach 100%, and the total recovery of the whole process reaches 52.7%.
Anion ligand promoted selective C-F bond reductive elimination enables C(sp2)-H fluorination
Mao, Yang-Jie,Luo, Gen,Hao, Hong-Yan,Xu, Zhen-Yuan,Lou, Shao-Jie,Xu, Dan-Qian
supporting information, p. 14458 - 14461 (2019/12/09)
A detailed mechanism study on the anion ligand promoted selective C-H bond fluorination is reported. The role of the anion ligand has been clarified by experimental evidence and DFT calculations. Moreover, the nitrate promoted C-F bond reductive elimination enabled a selective C-H bond fluorination of various symmetric and asymmetric azobenzenes to access diverse o-fluoroanilines.
A 3-amino-4-fluorophenylboronic acid synthesis method
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Paragraph 0022, (2016/11/24)
The invention discloses a synthetic method for 3-amino-4-fluorophenylboronic acid. The method includes the steps of conducting bromination on o-fluoronitrobenzene, conducting reduction to generate 5-bromo-2-fluoroanil, making 5-bromo-2-fluoroanil and tetrahydroxydiboron react in a coupled mode to generate the product, namely, 3-amino-4-fluorophenylboronic acid. According to the method, raw materials can be easily obtained, and operation is easy and convenient. The method is an appropriate route for preparing 3-amino-4-fluorophenylboronic acid.
Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT1F receptor agonists: Evolution from bicyclic to monocyclic cores
Zhang, Deyi,Blanco, Maria-Jesus,Ying, Bai-Ping,Kohlman, Daniel,Liang, Sidney X.,Victor, Frantz,Chen, Qi,Krushinski, Joseph,Filla, Sandra A.,Hudziak, Kevin J.,Mathes, Brian M.,Cohen, Michael P.,Zacherl, Deanna,Nelson, David L.G.,Wainscott, David B.,Nutter, Suzanne E.,Gough, Wendy H.,Schaus, John M.,Xu, Yao-Chang
, p. 4337 - 4341 (2015/11/03)
Preclinical experiments and clinical observations suggest the potential effectiveness of selective 5-HT1F receptor agonists in migraine. Identifying compounds with enhanced selectivity is crucial to assess its therapeutic value. Replacement of the indole nucleus in 2 (LY334370) with a monocyclic phenyl ketone moiety generated potent and more selective 5-HT1F receptor agonists. Focused SAR studies around this central phenyl ring demonstrated that the electrostatic and steric interactions of the substituent with both the amide CONH group and the ketone C=O group play pivotal roles in affecting the adopted conformation and thus the 5-HT1F receptor selectivity. Computational studies confirmed the observed results and provide a useful tool in the understanding of the conformational requirements for 5-HT1F receptor agonist activity and selectivity. Through this effort, the 2-F-phenyl and N-2-pyridyl series were also identified as potent and selective 5-HT1F receptor agonists.
CYCLOPROPANECARBOXAMIDO-SUBSTITUTE AROMATIC COMPOUNDS AS ANTI-TUMOR AGENTS
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Paragraph 0282; 0283, (2015/07/22)
Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.
CYCLOPROPANECARBOXAMIDO-SUBSTITUTE AROMATIC COMPOUNDS AS ANTI-TUMOR AGENTS
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Page/Page column 58, (2014/01/17)
Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.
Selective reduction of halogenated nitroarenes with hydrazine hydrate in the presence of Pd/C
Li, Fang,Frett, Brendan,Li, Hong-Yu
, p. 1403 - 1408 (2014/06/23)
A large variety of halogenated nitroarenes have been selectively reduced with hydrazine hydrate in the presence of Pd/C to give the corresponding (halogenated) anilines in good yield.
2-Pyrimidinyl Pyrazolopyridine ErbB Kinase Inhibitors
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Page/Page column 55; 80, (2009/06/27)
The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.
2-Pyrimidinyl Pyrazolopyridine Erbb Kinase Inhibitors
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Page/Page column 96; 112, (2008/06/13)
The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.
METHODS FOR PREPARING INDAZOLE COMPOUNDS
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Page/Page column 32, (2010/11/30)
The invention relates to methods for preparing compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof. Compounds of the formula (I) are useful as anti-angiogenesis agents and as agents for modulating and/or inhibiting the activity of protein kinases, thus providing treatments for cancer or other diseases associated with cellular proliferation mediated by protein kinases.