- Low-valent niobium-mediated double activation of C-F/C-H bonds: Fluorene synthesis from o-arylated α,α,α-trifluorotoluene derivatives
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By the treatment of 0.3 molar amount of NbCl5 and LiAlH4, o-arylated α,α,α-trifluorotoluenes afforded fluorene derivatives in good yields. C-F bonds of the CF3 group and the neighboring ortho C-H bond were doubly activated to give the coupling products. Copyright
- Fuchibe, Kohei,Akiyama, Takahiko
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Read Online
- A containing fluorophenylboronic acid production process
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The invention discloses a process for preparing fluorine-containing phenylboronic acid. The process comprises the following steps: 1) adding magnesium chips, borazine and an organic solvent into a reaction container; 2) adding an iodine initiator or a Grignard reagent, and stirring for 10-60min; 3) dripping a mixed solution of an organic solvent and a fluorine-containing phenyl compound within 1.5-2.5h for reacting, and controlling the temperature of the system to be between 20 DEG C and a reflux temperature; and 4) separating the reaction system of the last step and purifying to obtain the product. According to the process, the problems about stability and safety of a Grignard reagent intermediate in boronic acid production and ultralow-temperature operation are solved, the cost is reduced, the process is favorable for operation, and also the problem about compatibility of functional groups is also solved.
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Paragraph 0068; 0069; 0070
(2017/07/14)
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- Synthesis and evaluation of sulfonamide derivatives as potent Human Uric Acid Transporter 1 (hURAT1) inhibitors
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This letter presents synthesis and structure-activity relationship study of sulfonamide derivatives as inhibitors of Human Uric Acid Transporter 1 (hURAT1). Among all tested sulfonamide derivatives, compounds 9b, 16i and 19b exhibited excellent inhibition activity with IC50 value of 10, 2, and 83?nM, respectively. In addition, compounds 9b and 19b demonstrated moderate PK profile in rats.
- Yang, Xintuo,Pang, Xuehai,Fan, Lei,Li, Xinghai,Chen, Yuanwei
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supporting information
p. 1919 - 1922
(2017/04/10)
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- Nickel-catalyzed borylation of halides and pseudohalides with tetrahydroxydiboron [B2(OH)4]
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Arylboronic acids are gaining increased importance as reagents and target structures in a variety of useful applications. Recently, the palladium-catalyzed synthesis of arylboronic acids employing the atom-economical tetrahydroxydiboron (BBA) reagent has been reported. The high cost associated with palladium, combined with several limitations of both palladium- and copper-catalyzed processes, prompted us to develop an alternative method. Thus, the nickel-catalyzed borylation of aryl and heteroaryl halides and pseudohalides using tetrahydroxydiboron (BBA) has been formulated. The reaction proved to be widely functional group tolerant and applicable to a number of heterocyclic systems. To the best of our knowledge, the examples presented here represent the only effective Ni-catalyzed Miyaura borylations conducted at room temperature.
- Molander, Gary A.,Cavalcanti, Livia N.,Garcia-Garcia, Carolina
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p. 6427 - 6439
(2013/07/26)
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- OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS
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The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula (I), or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
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- Indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
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Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
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- Phenyl-isoxazoles as factor XA Inhibitors
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The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
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- Aryl- and arylamino- substituted heterocycles as corticotropin releasing hormone antagonists
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Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
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