24473-00-5Relevant academic research and scientific papers
A Stable Room-Temperature Luminescent Biphenylmethyl Radical
Ai, Xin,Chen, Yingxin,Feng, Yuting,Li, Feng
, p. 2869 - 2873 (2018)
There is only one family of room-temperature luminescent radicals, the triphenylmethyl radicals, to date. Herein, we synthesize a new stable room-temperature luminescent radical, (N-carbazolyl)bis(2,4,6-tirchlorophenyl)methyl radical (CzBTM), which has improved properties compared to the triphenylmethyl radicals. X-ray crystallography, electron paramagnetic resonance spectroscopy, and magnetic susceptibility measurements confirmed the radical structure. CzBTM shows room-temperature deep-red to near-infrared emission in various solutions. Both thermal and photo stability were significantly enhanced by the replacement of trichlorobenzene by the carbazole moiety. The electroluminescence results of CzBTM verify its potential application to circumvent the problem of triplet harvesting in traditional fluorescent OLEDs. A new family of stable luminescent radicals based on CzBTM is anticipated.
Monodentate Transient Directing Group Enabled Pd-Catalyzed Ortho-C-H Methoxylation and Chlorination of Benzaldehydes
Li, Feng,Zhou, Yirong,Yang, Heng,Wang, Ziqi,Yu, Qinqin,Zhang, Fang-Lin
supporting information, p. 3692 - 3695 (2019/05/24)
We report Pd-catalyzed ortho-C-H methoxylation and chlorination of benzaldehydes by employing monodentate transient directing groups (TDGs) as an alternative strategy to bidentate TDGs. More importantly, a single crystal of benzaldehyde imine ortho-cyclopalladium intermediate was successfully obtained, and its structure was unambiguously determined by X-ray diffraction, which clearly showed that it was a binuclear palladium species bridged by a pyridone ligand. The utility of this approach was further demonstrated through the synthesis of key intermediates of natural products and drugs.
A benzhydryl radical based on the room temperature of the organic light-emitting material and using the material preparation of organic electroluminescent device
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Paragraph 0025; 0026; 0027, (2018/07/30)
A benzhydryl radical based on the stability of the organic light-emitting material at room temperature and using the material preparation of the organic electroluminescent device, which belongs to the field of organic light-emitting technology. The present invention in the preparation of the organic light-emitting material, the center of the common characteristic is the carbon free radical, is composed of two C - C covalent bond and a C - N to form a covalent bond. Stability is the light-emitting free radical material in the application of the key nature, connected to the electronic group conducive to stable free radical, in this invention through the nitrogen-containing heterocyclic carbazole, indole, dimethyl acridine and the like in the electronic group to the nitrogen atom is connected directly to the benzyl group, to obtain a stable benzhydryl radical, its stability and PTM, compared with the TTM is greatly improved, and has a room temperature fluorescent. The preparation of the material of the organic electroluminescent device using double thread condition exciton light-emitting, can avoid the traditional organic electroluminescent device in the use of the triplet state exciton, the maximum external quantum efficiency of the device is 0.66%.
Small molecules inhibit STAT3 activation, autophagy, and cancer cell anchorage-independent growth
Zhou, Donghui,Springer, Maya Z.,Xu, David,Liu, Degang,Hudmon, Andy,Macleod, Kay F.,Meroueh, Samy O.
, p. 2995 - 3005 (2017/05/29)
Triple-negative breast cancers (TNBCs) lack the signature targets of other breast tumors, such as HER2, estrogen receptor, and progesterone receptor. These aggressive basal-like tumors are driven by a complex array of signaling pathways that are activated by multiple driver mutations. Here we report the discovery of 6 (KIN-281), a small molecule that inhibits multiple kinases including maternal leucine zipper kinase (MELK) and the non-receptor tyrosine kinase bone marrow X-linked (BMX) with single-digit micromolar IC50s. Several derivatives of 6 were synthesized to gain insight into the binding mode of the compound to the ATP binding pocket. Compound 6 was tested for its effect on anchorage-dependent and independent growth of MDA-MB-231 and MDA-MB-468 breast cancer cells. The effect of 6 on BMX prompted us to evaluate its effect on STAT3 phosphorylation and DNA binding. The compound's inhibition of cell growth led to measurements of survivin, Bcl-XL, p21WAF1/CIP1, and cyclin A2 levels. Finally, LC3B-II levels were quantified following treatment of cells with 6 to determine whether the compound affected autophagy, a process that is known to be activated by STAT3. Compound 6 provides a starting point for the development of small molecules with polypharmacology that can suppress TNBC growth and metastasis.
Diverse ortho-C(sp2)-H functionalization of benzaldehydes using transient directing groups
Liu, Xi-Hai,Park, Hojoon,Hu, Jun-Hao,Hu, Yan,Zhang, Qun-Liang,Wang, Bao-Long,Sun, Bing,Yeung, Kap-Sun,Zhang, Fang-Lin,Yu, Jin-Quan
supporting information, p. 888 - 896 (2017/05/16)
Pd-catalyzed C-H functionalizations promoted by transient directing groups remain largely limited to C-H arylation only. Herein, we report a diverse set of ortho-C(sp2)-H functionalizations of benzaldehyde substrates using the transient directing group strategy. Without installing any auxiliary directing group, Pd(II)-catalyzed C-H arylation, chlorination, bromination, and Ir(III)-catalyzed amidation, could be achieved on benzaldehyde substrates. The transient directing groups formed in situ via imine linkage can override other coordinating functional groups capable of directing C-H activation or catalyst poisoning, significantly expanding the scope for metal-catalyzed C-H functionalization of benzaldehydes. The utility of this approach is demonstrated through multiple applications, including late-stage diversification of a drug analogue.
SERINE RACEMASE INHIBITOR
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Paragraph 0145 - 0149, (2014/12/12)
A novel serine racemase inhibitor exhibits sufficient activity and specificity. The serine racemase inhibitor includes one or more compounds selected from compounds respectively represented by the following general formulas [MM_1], [DR_1], [DR'_1], [LW_1], and [ED_1] as an active ingredient.
PYRROLOPYRAZINE KINASE INHIBITORS
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Page/Page column 250; 251, (2013/03/28)
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
Monosubstituted malononitriles: Efficient one-pot reductive alkylations of malononitrile with aromatic aldehydes
Tayyari, Fariba,Wood, Dwight E.,Fanwick, Phillip E.,Sammelson, Robert E.
, p. 279 - 285 (2008/12/22)
A powerful new one-pot method has been developed for the reductive alkylation of malononitrile with aromatic aldehydes. This new procedure has vastly improved the yield and efficiency of the process, and increased the scope of the aromatic aldehydes. Inco
ACYLATED PIPERIDIHES AS GLYCINE TRANSPORTER INHIBITORS
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Page/Page column 50-51, (2010/11/23)
The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
1-(HETERO)ARYL-3-AMINO-PYROLLIDINE DERIVATIVES FOR USE AS MGLUR3 RECEPTOR ANTAGONISTS
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Page/Page column 74, (2010/11/08)
The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.
