64605-35-2Relevant academic research and scientific papers
Indole-3-carbonitriles as DYRK1A inhibitors by fragment-based drug design
Meine, Rosanna,Becker, Walter,Falke, Hannes,Preu, Lutz,Loa?c, Nadège,Meijer, Laurent,Kunick, Conrad
supporting information, (2018/02/07)
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a potential drug target because of its role in the development of Down syndrome and Alzheimer's disease. The selective DYRK1A inhibitor 10-iodo-11H-indolo[3, 2-c]quinoline-6-carboxy
Synergistic Cooperative Effect of Sodium borohydride-Iodine Towards Cascade C?N and C?S/Se Bond Formation: One-pot Regioselective Synthesis of 3-Sulfenyl/selenyl Indoles and Mechanistic Insight
Lavekar, Aditya G.,Equbal, Danish,Saima,Sinha, Arun K.
supporting information, p. 180 - 185 (2018/01/12)
In this work, a new strategy to synthesize 3-sulfenyl/selenyl indole is reported wherein LC?MS reveals a novel insight into synergistic cooperative effect of NaBH4-I2 which allows cascade C?N and C?S/C?Se bond formations via reduction-nucleophilic cyclization-chalcogenylation, three steps in one-pot, towards regioselective synthesis of diverse 3-chalcogenyl indoles including 5-bromo-3-[(3,4,5-trimethoxyphenyl)thio]-1H-indole, a known lead anticancer compound, directly from 2-amino-phenacylchlorides and thiophenols or disulfides/diselenides in aqueous dioxane under transition-metal-free condition. (Figure presented.).
N-(2-ARYLETHYL) BENZYLAMINES AS ANTAGONISTS OF THE 5-HT6 RECEPTOR
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Paragraph 0187, (2016/01/25)
The present invention relates to the use compounds of formula I which are antagonists of the 5-HT 6 receptor, for treating a cognitive disorder selected from the group consisting of age-related cognitive decline, mild cognitive impairment and dementia
[1,2]-Aryl migration in the synthesis of substituted indoles: scope, mechanism, and high throughput experimentation
Pei, Tao,Tellers, David M.,Streckfuss, Eric C.,Chen, Cheng-yi,Davies, Ian W.
experimental part, p. 3285 - 3291 (2009/08/08)
A mild regioselective synthesis of substituted indoles from readily accessible 1-(2-aminophenyl)-2-chloroethanones is described. Addition of a range of carbon nucleophiles to α-chloro acetophenones 1 generates 2-substituted indoles 2 in moderate to excell
Expanding the [1,2]-aryl migration to the synthesis of substituted indoles
Pei, Tao,Chen, Cheng-Yi,Dormer, Peter G.,Davies, Ian W.
, p. 4231 - 4233 (2008/12/23)
(Chemical Equation Presented) Closing in on the product: A range of 2- and 2,3-substituted indoles 2 have been synthesized in moderate to excellent yields by the addition of carbon nucleophiles (organometallic reagents, RM) to readily accessible 1-(2-aminophenyl)-2-chloroethanones of type 1 under mild conditions (see scheme). A mechanism has been proposed that involves a unique [1,2]-aryl migration of intermediate 3.
