- Method for catalytically synthesizing indole derivative by using ferrous complex
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The invention relates to a method for catalytically synthesizing an indole derivative by using a ferrous complex, which comprises the following step: by taking arylamine and acetaldehyde as raw materials and a ferrous complex containing a meta-carboboryl methylpyridine structure as a catalyst, conducting reacting at room temperature to prepare the indole derivative. Compared with the prior art, the method utilizes the ferrous complex to efficiently catalyze the reaction of arylamine and acetaldehyde at room temperature to prepare the indole derivative, the reaction condition is mild, the substrate range is wide, and the method has high catalytic activity and yield.
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Paragraph 0049-0052
(2021/07/31)
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- Decarboxylation of indole-3-carboxylic acids under metal-free conditions
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Two reaction systems have been developed for the decarboxylation of indole-3-carboxylic acids. The decarboxylation can be achieved smoothly under K2CO3-catalyzed or acetonitrile-promoted basic conditions. It provided an efficient and simple method for the transformation of indole-3-carboxylic acids and the corresponding indoles were isolated with good to excellent yields. From the experimental facts, we put forward the possible reaction mechanism.
- Chen, Xia,Zhou, Xiao-Yu
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supporting information
p. 805 - 812
(2020/02/20)
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- Method for synthesizing 7-nitroindole
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The invention relates to a method for synthesizing 7-nitroindole. The method comprises the following steps: subjecting oxime generated by condensation of o-nitroaniline, hydroxylamine and chloral to anucleophilic substitution reaction in a solvent under the action of an acidic substance and a drying agent, and performing hydrolyzing under alkaline conditions to generate an oximido intermediate; preparing 7-nitroisatin from the oximido intermediate in the presence of an acidic substance; and subjecting the 7-nitroisatin to reduction in a solvent by a system consisting of sodium borohydride andzirconium chloride so as to obtain the product 7-nitroindole. According to the method for synthesizing the 7-nitroindole, the product is obtained through three steps, so a production cycle is remarkably shortened and productivity is improved; used materials are simple and easily-available, so cost is low; reaction conditions are mild; the method is suitable for industrial mass production; meanwhile, the system of sodium borohydride and zirconium tetrachloride is used for replacing borane in the reduction step, so virulent, flammable and combustible raw materials are avoided, and the method issafer and environmentally friendlier.
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Paragraph 0010; 0020; 0022; 0023-0025
(2020/03/09)
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- Discovery of Potent Succinate-Ubiquinone Oxidoreductase Inhibitors via Pharmacophore-linked Fragment Virtual Screening Approach
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Succinate-ubiquinone oxidoreductase (SQR) is an attractive target for fungicide discovery. Herein, we report the discovery of novel SQR inhibitors using a pharmacophore-linked fragment virtual screening approach, a new drug design method developed in our laboratory. Among newly designed compounds, compound 9s was identified as the most potent inhibitor with a Ki value of 34 nM against porcine SQR, displaying approximately 10-fold higher potency than that of the commercial control penthiopyrad. Further inhibitory kinetics studies revealed that compound 9s is a noncompetitive inhibitor with respect to the substrate cytochrome c and DCIP. Interestingly, compounds 8a, 9h, 9j, and 9k exhibited good in vivo preventive effects against Rhizoctonia solani. The results obtained from molecular modeling showed that the orientation of the R2 group had a significant effect on binding with the protein.
- Xiong, Li,Zhu, Xiao-Lei,Gao, Hua-Wei,Fu, Yu,Hu, Sheng-Quan,Jiang, Li-Na,Yang, Wen-Chao,Yang, Guang-Fu
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p. 4830 - 4837
(2016/07/06)
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- Sweet anion receptors: Recognition of chiral carboxylate anions by d-glucuronic-acid-decorated diindolylmethane
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Anion receptors containing glucuronic acid were synthesized, and their anion binding ability studied. Chirality of anionic guests derived from mandelic acid and amino acids can be distinguished not only in terms of stability constants but also by signific
- Granda, Jaroslaw M.,Jurczak, Janusz
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supporting information
p. 4730 - 4733
(2013/10/08)
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- Benzenesulfonamide derivatives and pharmaceutical composition thereof
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The present invention is related to derivatives of benzenesulfonamide represented by formula (I), and the pharmaceutical composition thereof. In addition, the benzenesulfonamide derivatives disclosed in the present invention can serve as potential cell cycle inhibitors, and thereby these benzenesulfonamide derivatives and the pharmaceutical composition thereof can be antitumor drug candidates, which might aim at cell cycle. Particularly, the benzenesulfonamide derivatives disclosed in the present invention may function as antitumor drugs to treat solid cancers.
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Page/Page column 8; 10-11
(2011/10/10)
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- Pd-catalyzed conversion of aryl chlorides, triflates, and nonaflates to nitroaromatics
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(Chemical Equation Presented) An efficient Pd catalyst for the transformation of aryl chlorides, triflates, and nonaflates to nitroaromatics has been developed. This reaction proceeds under weakly basic conditions and displays a broad scope and excellent
- Fors, Brett P.,Buchwald, Stephen L.
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supporting information; experimental part
p. 12898 - 12899
(2009/12/07)
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- A new and efficient one-pot synthesis of indoles
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The synthesis of indoles is accomplished in high yields from phenylhydrazines and pyruvic acid using microwave irradiation.
- Bratulescu, George
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p. 984 - 986
(2008/09/17)
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- Synthesis, structure and the binding properties of the amide-based anion receptors derived from 1H-indole-7-amine
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Indole-7-amine was investigated as an alternative to aniline in construction of amide-based anion receptors. Replacement of aniline with indolamine introduces additional binding site-indolyl NH, which can enhance anion binding for more than five times. The molecular modelling of indole-containing receptors revealed the correlation between their conformational preferences and their affinity towards anions.
- Zieliński, Tomasz,Dydio, Pawe?,Jurczak, Janusz
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p. 568 - 574
(2008/04/12)
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- 7-Nitroindoles
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7-Aminoindole is prepared from a 7-nitroindole, which in turn is prepared from a halo-substituted β-dialkylamino-2-nitrostyrene.
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