- A class of indole derivatives and preparation methods and uses thereof
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The present invention relates to the field of medicinal chemistry, discloses a class of indole derivatives and preparation methods and uses thereof. The present invention also discloses a compound comprising the indole structure or a pharmaceutically acce
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Paragraph 0032; 0034-0036
(2022/01/12)
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- A Series of 2-((1-Phenyl-1H-imidazol-5-yl)methyl)-1H-indoles as Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors
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Indoleamine 2,3-dioxygenase 1 (IDO1) is a promising therapeutic target in cancer immunotherapy and neurological disease. Thus, searching for highly active inhibitors for use in human cancers is now a focus of widespread research and development efforts. I
- Zheng, Yong,Stafford, Paul M.,Stover, Kurt R.,Mohan, Darapaneni Chandra,Gupta, Mayuri,Keske, Eric C.,Schiavini, Paolo,Villar, Laura,Wu, Fan,Kreft, Alexander,Thomas, Kiersten,Raaphorst, Elana,Pasangulapati, Jagadeesh P.,Alla, Siva R.,Sharma, Simmi,Mittapalli, Ramana R.,Sagamanova, Irina,Johnson, Shea L.,Reed, Mark A.,Weaver, Donald F.
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supporting information
p. 2195 - 2205
(2021/05/31)
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- EIF4E INHIBITORS AND USES THEREOF
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The present invention provides compounds inhibiting elF4E activity and compositions and methods of using thereof.
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Paragraph 00337; 00
(2021/09/11)
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- Iodine-Mediated Electrochemical C(sp2)-H Amination: Switchable Synthesis of Indolines and Indoles
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A metal-free electrochemical intramolecular C(sp2)-H amination using iodine as a mediator was developed. This method enables a switchable synthesis of indoline and indole derivatives, respectively, from easily available 2-vinyl anilines.
- Hu, Kangfei,Zhang, Yan,Zhou, Zhenghong,Yang, Yu,Zha, Zhenggen,Wang, Zhiyong
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supporting information
p. 5773 - 5777
(2020/08/05)
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- Phenyl sulfide structure-containing compound or pharmaceutically acceptable salt, preparation method and application thereof
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The invention discloses a phenyl sulfide structure-containing compound with a structure as shown in a general formula (I) or pharmaceutically acceptable salt, a preparation method and application thereof. The compound containing the phenyl sulfide structu
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Paragraph 0040-0043
(2020/08/27)
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- Indole structure-containing compound or pharmaceutically acceptable salt, preparation method and application thereof
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The invention discloses an indole structure-containing compound with a structure as shown in a general formula (I) or pharmaceutically acceptable salt, a preparation method and application thereof. The indole structure-containing compound or the pharmaceu
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Paragraph 0043; 0045-0046
(2020/08/29)
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- Electron Transfer Photoredox Catalysis: Development of a Photoactivated Reductive Desulfonylation of an Aza-Heteroaromatic Ring
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Herein, we report a protocol for desulfonylation of aza-heteroaromatic rings via photoinduced electron transfer and hydrogen atom transfer. This general protocol has a wide substrate range and moderate to good yields. The utility of the method was demonstrated by the chemoselective desulfonylation of a molecule containing both an aliphatic and an aromatic sulfonamide. (Figure presented.).
- Qiang-Liu,Liu, Yu-Xiu,Song, Hong-Jian,Wang, Qing-Min
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supporting information
p. 3110 - 3115
(2020/07/04)
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- A 5 - cyano indole synthesis method (by machine translation)
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The invention relates to a 5 - cyano indole synthesis method, through to indole as the starting material, with sodium bisulfite reaction, and then sequentially by acetylation, brominated, protection, [...] and de-protected to obtain 5 - cyano indole. The present invention provides a method of synthesis of the price of raw materials is low cost and easily, thereby reducing the production cost. At the same time the invention synthetic route is short, high yield, high chemical purity of the obtained product, all the reactions are not need special production equipment, and the produced intermediate and final products are not needs the column chromatography and crystallization purification. So the invention not only reduces production cost, convenient for the industrial scale production; and can provide the market with high purity products, obtain the good economic benefits. (by machine translation)
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Paragraph 0060-0077
(2019/11/13)
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- N - substituted benzene sulfonyl -3 - propionyl indole derivatives, preparation method and application
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The invention discloses an N-substituted benzenesulfonyl-3-propionyl indole derivative, a preparation method and application and belongs to the technical field of organic synthesis. The structural formula of the N-substituted benzenesulfonyl-3-propionyl i
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Paragraph 0056-0060
(2018/07/30)
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- Preparation method of substituted indoles compounds
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The invention belongs to the field of medical technology, and discloses a preparation method of 3-substituted indoles compounds. The preparation method includes using a compound represented by formula (2) as an initial raw material, performing a Friedel-Crafts reaction with 4-chlorobutyryl chloride in the presence of anhydrous titanium tetrachloride catalyst to obtain a compound represented by formula (3), and performing a reaction with paratoluensulfonyl chloride in the presence of an organic solvent and an acid-binding agent to obtain the target compound. The preparation method overcomes the defects of the synthetic method in the prior art, and is suitable for the industrial production. The product has high content, and the purity of the product reaches over 99%.
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Paragraph 0021; 0022; 0023
(2016/10/07)
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- Flexible and practical synthesis of 3-oxyindoles through gold-catalyzed intermolecular oxidation of o-ethynylanilines
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A novel gold-catalyzed intermolecular oxidation of o-ethynylanilines has been developed. A range of functionalized 3-oxyindoles are readily accessed by utilizing this strategy. Importantly, this gold-catalyzed oxidative process outcompetes the typical ind
- Shu, Chao,Li, Long,Xiao, Xin-Yu,Yu, Yong-Fei,Ping, Yi-Fan,Zhou, Jin-Mei,Ye, Long-Wu
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supporting information
p. 8689 - 8692
(2014/07/22)
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- Synthesis and quantitative structure-activity relationship (QSAR) study of novel N-arylsulfonyl-3-acylindole arylcarbonyl hydrazone derivatives as nematicidal agents
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In continuation of our program aimed at the discovery and development of natural-product-based pesticidal agents, 54 novel N-arylsulfonyl-3-acylindole arylcarbonyl hydrazone derivatives were prepared, and their structures were well characterized by 1
- Che, Zhiping,Zhang, Shaoyong,Shao, Yonghua,Fan, Lingling,Xu, Hui,Yu, Xiang,Zhi, Xiaoyan,Yao, Xiaojun,Zhang, Rui
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p. 5696 - 5705
(2013/07/26)
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- Oxidative C-H/C-H coupling of azine and indole/pyrrole nuclei: Palladium catalysis and synthesis of eudistomin U
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We have developed a palladium-catalyzed C-H/C-H coupling reaction of indoles or pyrroles with azine N-oxides. The reaction proceeds selectively at the C3 position of indoles/pyrroles and the C2 position of azine N-oxides. Furthermore, we have accomplished
- Yamaguchi, Atsushi D.,Mandal, Debashis,Yamaguchi, Junichiro,Itami, Kenichiro
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supporting information; experimental part
p. 555 - 557
(2011/07/08)
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- Antifungal agents. Part 3: Synthesis and antifungal activities of 3-acylindole analogs against phytopathogenic fungi in vitro
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To find more potent antifungal compounds, twenty 3-acylindole analogs were synthesized and bio-evaluated for their antifungal activities against seven phytopathogenic fungi. Structure-activity relationships investigations revealed that 4- or 6-methyl and 3-acetyl or propionyl groups were the important structural properties of 3-acylindoles for the activities. Especially 4-methyl-3-propionylindole, 12, displayed the more potent activities than hymexazol, a commercially available agricultural fungicide, and might be considered as a new promising lead candidate for further design and synthesis of agricultural fungicides.
- Xu, Hui,Bin Yang, Wen,Wang, Qin
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experimental part
p. 864 - 868
(2012/06/29)
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- Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro
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In continuation of our program aimed at the discovery and development of compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 21N-arylsulfonyl-3-acetylindole analogs (2a-u) were synthesized and preliminarily evaluated as HIV-
- Ran, Jun-Qiang,Huang, Ning,Xu, Hui,Yang, Liu-Meng,Lv, Min,Zheng, Yong-Tang
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supporting information; experimental part
p. 3534 - 3536
(2010/08/21)
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- COPPER-CATALYZED FORMATION OF CARBON-HETEROATOM AND CARBON-CARBON BONDS
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One aspect of the present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-sulfur bond between the sulfur atom of a thiol moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper(II)-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-carbon bond between the carbon atom of cyanide ion and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In another embodiment, the present invention relates to a copper-catalyzed method of transforming and aryl, heteroaryl, or vinyl iodide. Yet another embodiment of the present invention relates to a tandem method, which may be practiced in a single reaction vessel, wherein the first step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl iodide from the corresponding aryl, heteroaryl, or vinyl chloride or bromide; and the second step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl nitrile, amide or sulfide from the aryl, heteroaryl, or vinyl iodide formed in the first step.
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- Glucagon antagonists/inverse agonists
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Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof are disclosed. The compounds act to antagonize the action of the glucagon peptide hormone.
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- Copper-catalyzed domino halide exchange-cyanation of aryl bromides
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An efficient copper-catalyzed domino halogen exchange-cyanation procedure for aryl bromides was developed utilizing 10 mol % CuI, 20 mol % KI, 1.0 equiv of the inexpensive N,N′-dimethylethylenediamine as ligand, and 1.2 equiv of NaCN in toluene at 110 °C. The new method represents a significant improvement over the traditional Rosenmund-von Braun reaction: the reaction conditions are much milder, and the use of stoichiometric amounts of copper(I) cyanide and polar solvents is avoided; therefore the isolation and purification of the aromatic nitrile products is greatly simplified. In addition, the new method exhibits excellent functional group compatibility comparable to that of the analogous Pd-catalyzed cyanation methodology. Copyright
- Zanon, Jacopo,Klapars, Artis,Buchwald, Stephen L.
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p. 2890 - 2891
(2007/10/03)
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- Neuroprotective indolone and related derivatives
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The present invention is directed to a method of blocking N-methyl-D-aspartic (NMDA) acid receptor sites in a mammal in need thereof with an effective NMDA blocking (neuroprotective and antiischemic) amount of 5-(1-hydroxy-2-piperidino)-propyl-2(1H,3H)-indolone analogs and the pharmaceutically acceptable salts thereof; methods of using these compounds in the treatment of stroke, head trauma, spinal cord trauma, traumatic brain injury, multiinfarct dementia, CNS degenerative diseases such as Alzheimer''s disease, senile dementia of the Alzheimer''s type, Huntington''s disease, Parkinson''s disease, epilepsy, amyotrophic lateral sclerosis, pain, AIDS dementia, psychotic conditions, drug addictions, migraine, hypoglycemia, anxiolytic conditions, urinary incontinence and an ischemic event arising from CNS surgery, open heart surgery or any procedure during which the function of the cardiovascular system is compromised.
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- Neuroprotective indolone and related derivatives
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5-(1-Hydroxy-2-piperidinopropyl)-2(1H,3H)-indolone derivatives and analogs; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.
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