27092-42-8Relevant academic research and scientific papers
Recyclable and reusablen-Bu4NBF4/PEG-400/H2O system for electrochemical C-3 formylation of indoles with Me3N as a carbonyl source
Cheng, Didi,Li, Jingyi,Li, Yujin,Ling, Fei,Liu, Lei,Liu, Tao,Zhong, Weihui
supporting information, p. 4107 - 4113 (2021/06/17)
A safe, practical and eco-friendly electrochemical methodology for the synthesis of 3-formylated indoles has been developed by the utilization of Me3N as a novel formylating reagent. Stoichiometric oxidants, metal catalysts, and activating agents were avoided in this method, and an aqueous biphasic system ofn-Bu4NBF4/PEG-400/H2O was used as a recyclable and reusable reaction medium, which made this electrosynthesis approach more sustainable and environmentally friendly. This process expanded the substrate scope and functional group tolerance for bothN-EDG andN-EWG indoles. Furthermore, late-stage functionalization and total/formal synthesis of drugs and natural products were realized by means of this route.
Spirocyclization reactions and antiproliferative activity of indole phytoalexins 1-methoxybrassinin and its 1-substituted derivatives
Budovská, Mariana,Pilátová, Martina Bago,Tischlerová, Viera,Moj?i?, Ján
, p. 198 - 234 (2017/09/25)
The effect of the reaction temperature and the solvent on the diastereoselectivity of the spirocyclization of 1-methoxybrassinin leading to 1-methoxyspirobrassinol methyl ether was studied. 1-Acyl derivatives of 1-methoxyspirobrassinol and 1-methoxyspirobrassinol methyl ether were prepared by the bromine-mediated spirocyclization reactions of derivatives of brassinin bearing an acyl group on the indole nitrogen with water or methanol as nucleophilic agents. The cyclization of 1-Acyl derivatives of brassinin afforded the trans-diastereoisomer as the major product, whereas using 1-methoxybrassinin afforded the cis-And trans-isomers in a ratio near to 1:1. Bromospirocyclization of brassinin and 1-methylbrassinin in the presence of methanol resulted in the formation of spirobrassinin and 1-methylspirobrassinin. The newly synthesized analogues of indole phytoalexins exhibited more significant antiproliferative activity against human leukemia cell lines than the natural phytoalexins.
COMPOSITIONS AND METHODS FOR TARGETING RECEPTORS EXPRESSED IN THE GUT
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Page/Page column 39; 40, (2016/02/09)
The invention relates to novel compounds and pharmaceutical preparations thereof, as well as methods of making and using these compounds. The invention further relates to methods of treating or preventing disease using the novel compounds of the invention
Spirocyclization reactions and antiproliferative activity of indole phytoalexins 1-methoxybrassinin and its 1-substituted derivatives
Budovská, Mariana,Pilátová, Martina Bago,Tischlerová, Viera,Moj?i?, Ján
, p. 198 - 234 (2018/05/09)
The effect of the reaction temperature and the solvent on the diastereoselectivity of the spirocyclization of 1-methoxybrassinin leading to 1-methoxyspirobrassinol methyl ether was studied. 1-Acyl derivatives of 1-methoxyspirobrassinol and 1-methoxyspirobrassinol methyl ether were prepared by the bromine-mediated spirocyclization reactions of derivatives of brassinin bearing an acyl group on the indole nitrogen with water or methanol as nucleophilic agents. The cyclization of 1-acyl derivatives of brassinin afforded the trans-diastereoisomer as the major product, whereas using 1-methoxybrassinin afforded the cis- and trans-isomers in a ratio near to 1:1. Bromospirocyclization of brassinin and 1-methylbrassinin in the presence of methanol resulted in the formation of spirobrassinin and 1-methylspirobrassinin. The newly synthesized analogues of indole phytoalexins exhibited more significant antiproliferative activity against human leukemia cell lines than the natural phytoalexins.
POLYMERASE, ENDONUCLEASE, AND HELICASE INHIBITORS AND METHODS OF USING THEREOF
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Paragraph 0169, (2014/11/13)
Inhibitors of DNA damage polymerases, endonucleases, and helicases are provided. In particular, compounds comprising Formula (I) are described.
Synthesis and biological evaluation of curcumin analogues having a piperidone core as potential antioxidant agents
Wang, Jian,Sun, Gangchun,Li, Zhicheng,Mai, Wenpeng,Xie, Jingxi
experimental part, p. 63 - 65 (2012/05/19)
A series of new unsymmetrical curcumin derivatives were designed and synthesised to which the indole fragment was introduced according to the principle of association. These compounds were characterised by 1H NMR, IR, ESIMS and elemental analys
N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: Synthesis and biological evaluation
Kaur, Jatinder,Bhardwaj, Atul,Huang, Zhangjian,Knaus, Edward E.
experimental part, p. 2154 - 2159 (2012/04/18)
A group of N-1 and C-3 disubstituted-indole Schiff bases bearing an indole N-1 (R′ = H, CH2Ph, COPh) substituent in conjunction with a C-3 -CHN-C6H4-4-X (X = F, Me, CF3, Cl) substituent were synthesized and eval
NBu4NI-catalyzed C3-formylation of indoles with N-methylaniline
Li, Lan-Tao,Huang, Juan,Li, Hong-Ying,Wen, Li-Juan,Wang, Peng,Wang, Bin
supporting information; experimental part, p. 5187 - 5189 (2012/06/01)
nBu4NI-catalyzed C3-selective formylation of N-H and N-substituted indoles by using N-methylaniline as a formylating reagent was first successfully demonstrated.
Synthesis and evaluation of indole, pyrazole, chromone and pyrimidine based conjugates for tumor growth inhibitory activities - Development of highly efficacious cytotoxic agents
Singh, Palwinder,Kaur, Matinder,Holzer, Wolfgang
experimental part, p. 4968 - 4982 (2010/11/20)
Based upon the lead compounds 10 and 11, a number of conjugates were synthesized by the combination of chromone-pyrimidine, chromone-indolinone, chromone-pyrazole, indole-pyrimidine, indole-indolinone and indole-pyrazole moieties. Evaluation of these compounds for tumor growth inhibitory activities over 60 human tumor cell lines provided highly efficacious compounds 15, 41, 43, 66, 69, and 72 with an average GI50 over all the 60 human tumor cell lines as 3.2 μM, 3.1 μM, 1.7 μM, 2.6 μM, 50.1 μM and 2.0 μM, respectively.
A catalytic antibody programmed for torsional activation of amide bond hydrolysis
Aggarwal, Ranjana,Benedetti, Fabio,Berti, Federico,Buchini, Sabrina,Colombatti, Alfonso,Dinon, Francesca,Galasso, Vinicio,Norbedo, Stefano
, p. 3132 - 3142 (2007/10/03)
Amidase antibody 312d6, obtained against the sulfonamide hapten 4a that mimics the transition state for hydrolysis of a distorted amide, accelerates the hydrolysis of the corresponding amides 1a-3a by a factor of 103 at pH 8. The mechanisms of
