944086-13-9Relevant academic research and scientific papers
Rh(III)-Catalyzed [5 + 1] Annulation of Indole-enaminones with Diazo Compounds to Form Highly Functionalized Carbazoles
Jiang, Zhidong,Liu, Hong,Zhou, Jianhui,Zhou, Yu,Zhu, Haoran
supporting information, p. 4406 - 4410 (2021/06/28)
A novel Rh(III)-catalyzed C-H activation/annulation cascade of indole-enaminones with diazo compounds was reported to construct diversely functionalized carbazole frameworks. The most notable characteristic is that this transformation could smoothly furnish a novel [5 + 1] cyclization product with good to excellent yields (up to 95%), accompanied by the thorough removal of acetyl and N,N-dimethyl groups of two substrates from the target products, rather than the normally expected [4 + 2] cyclization products.
Cascade Reaction to Selectively Synthesize Multifunctional Indole Derivatives by IrIII-Catalyzed C?H Activation
Chai, Xin-Yue,Xu, Hui-Bei,Dong, Lin
supporting information, p. 13123 - 13127 (2021/08/13)
An effective and condition-controlled way to synthesize with high selectivity a variety of functionalized indoles with potent biological properties has been developed. Notably, 2,4-dialkynyl indole products were obtained by direct double C?H bond alkynylation, whereas alkynyl at the C4 position could convert to carbonyl to generate 2-alkynyl-3,4-diacetyl indoles fast and effectively. Additionally, a one-pot relay catalytic reaction led to 2,5-di-alkynyl-3,4-diacetyl indoles when using a carbonyl group as the directing group and by controlling the type and quantity of additives. A possible mechanism was proposed based on many studies including deuterium-exchange experiments, the necessary conditions of product conversion, and the effect of water on the reaction.
Palladium-catalyzed regioselective C-H fluoroalkylation of indoles at the C4-position
Borah, Arun Jyoti,Shi, Zhuangzhi
supporting information, p. 3945 - 3948 (2017/04/11)
An exclusive catalytic C4-selective fluoroalkylation of indoles with highly active (1H, 1H-perfluoroalkyl)mesityliodonium triflate has been described. The key to its high regioselectivity is the appropriate choice of an easily accessible, cheap and removable directing group at the C3 position in the presence of a Pd(OAc)2 catalyst. Besides indole fluoroalkylation, the application of this strategy in other heteroarenes such as benzo[b]thiophene is also described.
A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series
De Luca, Laura,Barreca, Maria Letizia,Ferro, Stefania,Iraci, Nunzio,Michiels, Martine,Christ, Frauke,Debyser, Zeger,Witvrouw, Myriam,Chimirri, Alba
, p. 2891 - 2895 (2008/12/21)
We report herein the development of a new three-dimensional pharmacophore model for HIV-1 integrase inhibitors which led to the discovery of some 4-[1-(4-fluorobenzyl)-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acids that are able to specifically inhibit the strand transfer step of integration at nanomolar concentration. The synthesis of the new designed molecules is also described.
BICYCLIC NITROGEN COMPOUNDS AS MODULATORS OF GHRELIN RECEPTOR AND USES THEREOF
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Page/Page column 79, (2010/11/28)
Disclosed herein are compounds of Formula I as defined herein, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, that modulates the activity of a ghrelin receptor. Disclosed herein are also methods of treating diseases or conditions that comprise administering to a subject in need thereof a therapeutically effective amount of a compound of Formula I.
