945000-95-3Relevant academic research and scientific papers
Palladium-Catalyzed Direct C2-Biarylation of Indoles
Murugesan, Tamilarasu,Sivarajan, Chinraj,Jayakumari, Chithra Mohan,Singh, Rajat Kumar,Vennapusa, Sivaranjana Reddy,Kaliyamoorthy, Alagiri
supporting information, p. 10838 - 10851 (2021/08/16)
Biaryl and indole units are important structural motifs in several bioactive molecules and functional materials. We have accomplished straightforward access to C2-biarylated indole derivatives through palladium-catalyzed C-H activation strategy with a bro
NH4I/1,10-phenanthroline catalyzed direct sulfenylation of N-heteroarenes with ethyl arylsulfinates
Chen, Lingjuan,Zhang, Jun,Wei, Yueting,Yang, Zhen,Liu, Ping,Zhang, Jie,Dai, Bin
, (2019/10/14)
An efficient synthesis of N-heterocyclic aryl sulfides via NH4I/1,10-phenanthroline-catalyzed direct sulfenylation reactions was reported. In this reaction, heteroarenes such as indoles, and pyrroles serve as nucleophiles by installing a arylthio group at the C3 and C2 position of heterocycles, respectively. With readily accessible and free of unpleasant odor ethyl arylsulfinates as sulfur reagents, the metal-free-catalyzed direct sulfenylation of N-heteroarenes has been developed. 3-Arylthio-indoles and 2-arylthio-pyrroles derivatives were obtained in moderate to excellent yields, even on gram scale. The reaction was general for a broad scope of substrates and demonstrated good tolerance to a variety of functional groups.
Palladium-Catalyzed Oxidative Sulfenylation of Indoles and Related Electron-Rich Heteroarenes with Aryl Boronic Acids and Elemental Sulfur
Li, Jianxiao,Li, Chunsheng,Yang, Shaorong,An, Yanni,Wu, Wanqing,Jiang, Huanfeng
, p. 7771 - 7783 (2016/09/12)
An efficient and convenient palladium-catalyzed C-H bond oxidative sulfenylation of indoles and related electron-rich heteroarenes with aryl boronic acids and elemental sulfur has been described. This procedure provides a useful and direct approach for the assembly of a wide range of structurally diverse 3-sulfenylheteroarenes with moderate to excellent yields from simple and readily available starting materials. Moreover, this synthetic protocol is suitable for N-protected and unprotected indoles. Notably, the construction of two C-S bonds in one step was also achieved in this transformation.
Dual acting norepinephrine reuptake inhibitors and 5-HT2A receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles
Heffernan, Gavin D.,Coghlan, Richard D.,Manas, Eric S.,McDevitt, Robert E.,Li, Yanfang,Mahaney, Paige E.,Robichaud, Albert J.,Huselton, Christine,Alfinito, Peter,Bray, Jenifer A.,Cosmi, Scott A.,Johnston, Grace H.,Kenney, Thomas,Koury, Elizabeth,Winneker, Richard C.,Deecher, Darlene C.,Trybulski, Eugene J.
experimental part, p. 7802 - 7815 (2010/03/24)
The discovery of a series of 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles, dual acting norepinephrine reuptake inhibitors (NRIs) and 5-HT2A receptor antagonists, is described. The synthesis and structure-activity relationship (SAR) of this novel
SULFONYL SUBSTITUTED 1H-INDOLES AS LIGANDS FOR THE 5-HYDROXYTRYPTAMINE RECEPTORS
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Page/Page column 92, (2008/06/13)
The present invention is directed to compounds of Formula I: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the invention, and pharmaceutical comp
