- Catalytic Synthesis of Atropisomeric o-Terphenyls with 1,2-Diaxes via Axial-to-Axial Diastereoinduction
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Herein, we report a modular and convergent strategy for the assembly of atropisomeric o-terphenyls with 1,2-diaxes via palladium/chiral norbornene cooperative catalysis and axial-to-axial diastereoinduction. Readily available aryl iodides, 2,6-substituted aryl bromides, and potassium aryl trifluoroborates are used as the building blocks, laying the foundation for diversity-oriented synthesis of these scaffolds (46 examples). Other features include the unique axial-to-axial diastereoinduction mode, construction of two axes in a single operation, and step economy. DFT calculations are performed to rationalize the axial-to-axial diastereoinduction process. Synthetic utilities of this method in preparation of atropisomeric oligophenyls, chiral catalysts, and ligands are demonstrated.
- Gao, Qianwen,Wu, Chenggui,Deng, Shuang,Li, Lisha,Liu, Ze-Shui,Hua, Yu,Ye, Jinxiang,Liu, Chang,Cheng, Hong-Gang,Cong, Hengjiang,Jiao, Yinchun,Zhou, Qianghui
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Read Online
- 1, 1 '-biphenyl-2, 6-diphenol compound and application thereof
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The invention discloses a 1, 1 '-biphenyl-2, 6-diphenol compound and application thereof, and the 1, 1'-biphenyl-2, 6-diphenol compound is a new compound and has good biological activity. Through an in-vitro tumor cell activity experiment method, it is fo
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Paragraph 0044; 0046
(2021/03/18)
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- C-H borylation by platinum catalysis
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Herein, we describe the platinum-catalyzed borylation of aromatic C-H bonds. N-Heterocyclic carbene-ligated platinum catalysts are found to be efficient catalysts for the borylation of aromatic C(sp2)-H bonds when bis(pinacolato)diboron is used as the boron source. The most remarkable feature of these Pt catalysts is their lack of sensitivity towards the degree of steric hindrance around the C-H bonds undergoing the borylation reaction. These Pt catalysts allow for the synthesis of sterically congested 2,6-disubstituted phenylboronic esters, which are otherwise difficult to synthesize using existing C-H borylation methods. Furthermore, platinum catalysis allows for the site-selective borylation of the C-H bonds ortho to fluorine substituents in fluoroarene systems. Preliminary mechanistic studies and work towards the synthetic application of this platinum catalyzed C-H borylation process are described.
- Furukawa, Takayuki,Tobisu, Mamoru,Chatani, Naoto
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supporting information
p. 332 - 342
(2017/05/09)
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- Design and Discovery of N-(2-Methyl-5′-morpholino-6′-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers
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RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant tumors has been established in genetically engineered mouse models and human tumor cells. To date
- Nishiguchi, Gisele A.,Rico, Alice,Tanner, Huw,Aversa, Robert J.,Taft, Benjamin R.,Subramanian, Sharadha,Setti, Lina,Burger, Matthew T.,Wan, Lifeng,Tamez, Victoriano,Smith, Aaron,Lou, Yan,Barsanti, Paul A.,Appleton, Brent A.,Mamo, Mulugeta,Tandeske, Laura,Dix, Ina,Tellew, John E.,Huang, Shenlin,Mathews Griner, Lesley A.,Cooke, Vesselina G.,Van Abbema, Anne,Merritt, Hanne,Ma, Sylvia,Gampa, Kalyani,Feng, Fei,Yuan, Jing,Wang, Yingyun,Haling, Jacob R.,Vaziri, Sepideh,Hekmat-Nejad, Mohammad,Jansen, Johanna M.,Polyakov, Valery,Zang, Richard,Sethuraman, Vijay,Amiri, Payman,Singh, Mallika,Lees, Emma,Shao, Wenlin,Stuart, Darrin D.,Dillon, Michael P.,Ramurthy, Savithri
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supporting information
p. 4869 - 4881
(2017/06/28)
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- TRICYCLIC COMPOUND AND USE THEREOF
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The present invention relates to: a compound selected from the group consisting of a tricyclic compound having the structure of formula I, a pharmaceutically acceptable salt, an isomer, a solvate and a precursor thereof; and a use thereof. The compound effectively controls GPR40, and thus, can be effectively used for the prophylaxis or treatment of diseases associated with GPR40, for example, diabetes and many other diseases.
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Paragraph 0470; 0471; 0472
(2016/01/25)
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- HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS AND COMBINATIONS THEREOF
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Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
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- BORON-CONTAINING DIACYLHYDRAZINES
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The present disclosure provides boron-containing diacylhydrazines having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, and R5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.
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- HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS
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Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.
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- A benzoboroxole-functionalized monolithic column for the selective enrichment and separation of cis-diol containing biomolecules
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A benzoboroxole-functionalized monolithic column was synthesized, which exhibited the best specificity and affinity towards cis-diol containing biomolecules as compared with the boronate affinity monolithic columns reported as well as significant secondar
- Li, Hengye,Wang, Heye,Liu, Yunchun,Liu, Zhen
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supporting information; experimental part
p. 4115 - 4117
(2012/06/16)
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- Palladium-catalyzed borylation of aryl arenesulfonates with dialkoxyboranes
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The cross-coupling of aryl arenesulfonates with dialkoxyboranes proceeded in the presence of Bu4NI and a catalytic amount of [Pd(dba) 2]/1,1'-bis(di-tert-butylphosphano)ferrocene, giving good yields of the corresponding arylboronates. The protocols tolerate a wide range of functional groups, including ester, nitrile, and ketone.
- Murata, Miki,Oda, Takeshi,Sogabe, Yosuke,Tone, Hirofumi,Namikoshi, Takeshi,Watanabe, Shinji
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p. 962 - 963
(2011/12/05)
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- COMPOUND HAVING 6-MEMBERED AROMATIC RING
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An object of the present invention is to provide an agent for preventing or treating schizophrenia or the like, wherein the compound of the present invention has GPR52 agonist activity. [Means] A compound represented by the following formula (I) or salt t
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Page/Page column 49
(2010/12/17)
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