- Method for synthesizing benzoxazole through microwave radiation of benzamide compound in water phase
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The invention discloses a method for synthesizing benzoxazole through microwave radiation of a benzamide compound in a water phase. The benzamide compound is added into the water phase under the microwave condition to be subjected to a cyclization reaction for generating the benzoxazole under the alkali condition, and the method for preparing the benzoxazole is environmentally friendly, easy and convenient to operate, safe, low in cost and efficient. Compared with the prior art, the method can be applied to a large number of functional groups, the yield is high, the number of by-products is small, and the method is easy to operate, safe, low in cost and environmentally friendly. (Please see the specifications for the formula).
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Paragraph 0075
(2019/03/08)
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- HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS
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Aminopyrazine compounds as modulators of an adenosine receptor are provided. The compounds may find use as therapeutic agents for the treatment of diseases mediated through a G-protein-coupled receptor signaling pathway and may find particular use in oncology.
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Paragraph 0390; 0393; 0394
(2019/02/05)
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- 1,8-NAPHTHYRIDINONE COMPOUNDS AND USES THEREOF
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1,8-naphthyridinone compounds as modulators of an adenosine receptor are provided. The compounds may find use as therapeutic agents for the treatment of diseases mediated through a G-protein-coupled receptor signaling pathway and may find particular use in oncology.
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Paragraph 0350; 0355; 0356
(2019/02/05)
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- Cobalt-catalyzed synthesis of N-containing heterocycles: Via cyclization of ortho -substituted anilines with CO2/H2
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The CO2-involved synthesis of chemicals is of great significance from the green and sustainable chemistry viewpoint. Herein, we report a non-noble metal catalytic system composed of CoF2, CsF and P(CH2CH2PPh2)3 (denoted as PP3) for the synthesis of N-containing heterocycles from ortho-substituted anilines and CO2/H2. Mechanism investigation indicates that [Co(PP3)H(CO2)]+ is a catalytically active intermediate under working conditions; and CsF plays important roles in activating ortho-substituted anilines via hydrogen bond interactions, thus promoting the formation of the final products. This catalytic system is highly efficient, and allows a wide scope of ortho-substituted anilines, together with excellent functional group tolerance, affording various N-containing heterocycles in good to excellent yields.
- Ke, Zhengang,Yu, Bo,Wang, Huan,Xiang, Junfeng,Han, Juanjuan,Wu, Yunyan,Liu, Zhenghui,Yang, Peng,Liu, Zhimin
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p. 1695 - 1701
(2019/04/10)
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- Room-temperature palladium-catalyzed direct 2-alkenylation of azole derivatives with alkenyl bromides
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Pd-catalyzed direct C2-alkenylation of azole derivatives proceeds efficiently under mild conditions, and the reaction of substituted benzoxazoles, oxazole and benzothiazole occurred even at room temperature. The substrate scope of the reaction was turned out to include mono-, di- and trisubstituted alkenyl bromides. To validate the scalability of this method, 5-Methyl-2-(prop-1-en-2-yl)benzoxazole (3c) was prepared on one-gram scale at room temperature.
- Yao, Yun-Xin,Fang, Dong-Mei,Gao, Feng,Liang, Xiao-Xia
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supporting information
p. 68 - 71
(2018/12/05)
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- Cu-Catalyzed Direct C-P Bond Formation through Dehydrogenative Cross-Coupling Reactions between Azoles and Dialkyl Phosphites
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A direct dehydrogenative cross-coupling of azoles [C(sp2)-H] with dialkyl phosphites [P(O)-H] to access 2-phosphonated azoles using Cu(I)/Cu(II) as catalyst and K2S2O8/di-tert-butylperoxide as oxidant has been achieved. A remarkable advantage over reported procedures includes that oxazoles, imidazoles, benz(ox/othi/imid)azoles, and indole are found to react under optimized reaction conditions to provide corresponding adducts in high yields. The mechanistic insight of cross-coupling was obtained by deuterium kinetic isotope effect studies.
- Hore, Soumyadip,Srivastava, Abhijeet,Singh, Ravi P.
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p. 6868 - 6878
(2019/06/14)
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- 1H-[1,2,3]triazolo[4,5-c]quinoline derivative, preparation method and uses thereof
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The invention belongs to the field of chemical medicine, particularly relates to a 1H-[1,2,3]triazolo[4,5-c]quinoline derivative, a preparation method and uses thereof, and provides a 1H-[1,2,3]triazolo[4,5-c]quinoline derivative, which has a structure represented by a formula I. The invention further provides a preparation method and uses of the 1H-[1,2,3]triazolo[4,5-c]quinoline derivative. Theformula I is defined in the specification.
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Paragraph 0316; 0317; 0318; 0319
(2018/09/28)
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- Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers
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Autophagy inducers represent new promising agents for the treatment of a wide range of medical illnesses. However, safe autophagy inducers for clinical applications are lacking. Inhibition of cdc2-like kinase 1 (CLK1) was recently found to efficiently induce autophagy. Unfortunately, most of the known CLK1 inhibitors have unsatisfactory selectivity. Herein, we report the discovery of a series of new CLK1 inhibitors containing the 1H-[1,2,3]triazolo[4,5-c]quinoline scaffold. Among them, compound 25 was the most potent and selective, with an IC50 value of 2 nM against CLK1. The crystal structure of CLK1 complexed with compound 25 was solved, and the potency and kinase selectivity of compound 25 were interpreted. Compound 25 was able to induce autophagy in in vitro assays and displayed significant hepatoprotective effects in the acetaminophen (APAP)-induced liver injury mouse model. Collectively, due to its potency and selectivity, compound 25 could be used as a chemical probe or agent in future mechanism-of-action or autophagy-related disease therapy studies.
- Sun, Qi-Zheng,Lin, Gui-Feng,Li, Lin-Li,Jin, Xi-Ting,Huang, Lu-Yi,Zhang, Guo,Yang, Wei,Chen, Kai,Xiang, Rong,Chen, Chong,Wei, Yu-Quan,Lu, Guang-Wen,Yang, Sheng-Yong
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p. 6337 - 6352
(2017/08/02)
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- Cobalt-Catalyzed Cross-Dehydrogenative Coupling Reactions of (Benz)oxazoles with Ethers
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The cobalt-catalyzed cross-dehydrogenative coupling of (benz)oxazoles and ethers is described. Access to some important bioactive heteroaryl ether derivatives was achieved using CoCO3 as an inexpensive catalyst at levels as low as 1.0 mol %. In
- Li, Yanrong,Wang, Mengshi,Fan, Wei,Qian, Fen,Li, Guigen,Lu, Hongjian
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p. 11743 - 11750
(2016/12/09)
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- HETEROCYCLIC COMPOUNDS AS CALCIUM SENSING RECEPTOR MODULATORS FOR THE TREATMENT OF HYPERPARATHYROIDISM, CHRONIC RENAL FAILURE AND CHRONIC KIDNEY DISEASE
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The invention relates to heterocyclic compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their pharmaceutical compositions for use in medicine for the treatment of diseases or disorders associated with the modulation of calcium sensing receptor modulators (CaSR), like e.g. hyperparathyroidism, chronic renal failure and chronic kidney disease and their complications.
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Page/Page column 47
(2015/11/16)
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- Direct C-H iodination of 1,3-azoles catalysed by CuBr2
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A mild method was developed for the direct C-H iodination of 1,3-azoles catalysed by CuBr2. Compared with the traditional metalation/iodination sequences carried out with nBuLi or TMPLi (TMP = 2,2,6,6-tetramethylpiperidino), a relatively weaker base, LiOtBu, was used in the presence of 1,10-phenanthroline. Five series of 1,3-azoles, including benzoxazole, benzothiozole, N-methyl-benzoimidazole, 5-phenyloxazole and 2-phenyl-1,3,4-oxadiazole were tested and afforded the corresponding iodination products.
- Zhao, Xia,Ding, Fang,Li, Jingyu,Lu, Kui,Lu, Xiaoyu,Wang, Bin,Yu, Peng
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supporting information
p. 511 - 513
(2015/02/19)
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- Copper-catalyzed oxidative decarboxylative C-H arylation of benzoxazoles with 2-nitrobenzoic acids
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A copper-catalyzed oxidative decarboxylative coupling of benzoxazoles with 2-nitrobenzoic acids was developed. This methodology favors electron-rich benzoxazoles and electron-deficient benzoic acids and enables the preparation of a variety of arylated benzoxazoles in good yields. The trends in product yields suggest a delicate balance between the decarboxylation and C-H arylation steps.
- Chen, Lijun,Ju, Lin,Bustin, Katelyn A.,Hoover, Jessica M.
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supporting information
p. 15059 - 15062
(2015/10/12)
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- GAMMA-DIKETONES AS WNT/BETA -CATENIN SIGNALING PATHWAY ACTIVATORS
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The present disclosure provides γ-diketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
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Paragraph 1741; 1742
(2014/09/03)
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- Copper-catalyzed oxidative amination of benzoxazoles via C-H and C-N bond activation: A new strategy for using tertiary amines as nitrogen group sources
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An efficient and conceptually new method for oxidative amination of azoles with tertiary amines via copper-catalyzed C-H and C-N bond activation has been developed. This protocol can be performed in the absence of external base and only requires atmospheric oxygen as oxidant. The catalyst system is very simple and efficient, which opens a new way for using tertiary amines as nitrogen group sources for C-N bond formation reactions.
- Guo, Shengmei,Qian, Bo,Xie, Yinjun,Xia, Chungu,Huang, Hanmin
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experimental part
p. 522 - 525
(2011/04/18)
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- CALCIUM RECEPTOR MODULATING ARYLALKYLAMINES
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The compounds of the invention are represented by the following general structure (I) or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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