134903-48-3

Upstream product

• 487-89-8 Indole-3-carboxaldehyde 
• 1973-22-4 1-bromo-2-ethylbenzene 
• 1213706-95-6 C₁₇H₁₄INO 
• 103-63-9 1-phenyl-2-bromoethane 
• 119910-45-1 2-bromo-1H-indole-3-carbaldehyde 
• 120-72-9 indole 
• 10006-87-8 1-phenethyl-1H-indole 
• 68-12-2 N,N-dimethyl-formamide 
• 139409-34-0 2-bromo-1H-indole 
• 288848-93-1 2-bromo-1-phenethyl-1H-indole-3-carbaldehyde 

Relevant academic research and scientific papers

Synthesis, antimycobacterial and anticancer activity of novel indole-based thiosemicarbazones

Based on the structural elements of bioactive indole-based compounds, a series of novel 1-substituted indole-3-carboxaldehyde thiosemicarbazones were synthesized as potential antimycobacterial and anticancer agents. The derivatives were prepared via a two

Selective and Efficient Formylation of Indoles (C3) and Pyrroles (C2) Using 2,4,6-Trichloro-1,3,5-Triazine/Dimethylformamide (TCT/DMF) Mixed Reagent

This study introduces an efficient method for the selective formylation of indoles and pyrroles at the positions of C(3) and C(2), respectively. The mixture of three equivalents of N,N-dimethylformamide and one equivalent of 2,4,6-trichloro-1,3,5-triazine (cyanuric chloride) generates an easy handling formylating agent for the efficient formylation of these classes of compounds to give the corresponding aldehydes under mild reaction conditions. This procedure was highly efficient, and a range of formylated indoles and pyrroles were obtained in good to excellent yields.

B-ring modified aurones as promising allosteric inhibitors of hepatitis C virus RNA-dependent RNA polymerase

Following our recent report showing the potential of naturally occurring aurones (2-benzylidenebenzofuran-3(2H)-ones) as anti-hepatitis C virus (HCV) agents, efforts were continued in order to refine the structural requirements for the inhibitory effect on HCV RNA-dependent RNA polymerase (RdRp). In this study, we targeted the B-ring moiety of aurones with the aim to improve structural features associated with higher inhibition of the targeted polymerase. In vitro evaluation of the RdRp inhibitory activity of the 37 newly synthesized compounds pointed out that the replacement of the B-ring with an N-substituted indole moiety induced the highest inhibitory effect. Of these, compounds 31, 40 and 41 were found to be the most active (IC50 = 2.3-2.4 μM). Docking experiments performed with the most active compounds revealed that the allosteric thumb pocket I of RdRp is the binding pocket for aurone analogues.

Intramolecular oxidative C-H coupling for medium-ring synthesis

An oxidative C-H coupling is described for medium-ring synthesis.

Intramolecular photochemical cross-coupling reactions of 3-acyl-2-haloindoles and 2-chloropyrrole-3-carbaldehydes with substituted benzenes

Highly efficient syntheses of indolo[2,1-a]isoquinolines, indolo[2,1-a][2]benzazepines, pyrrolo[2,1-a]isoquinolines and pyrrolo[1,2-a]benzazepines in excellent yields have been achieved by the intramolecular photochemical cross-coupling reactions of 3-acyl-2-halo-N- (ω-arylalkyl)indoles and 2-chloro-N-(ω-arylalkyl)pyrrole-3- carbaldehydes in acetone. A new heterocyclic ring system - pyrrolo[1,2-d][1,4] benzoxazepine - has also been constructed for the first time in this work by the photocyclization of 2-chloro-N-(2-phenoxyethyl)pyrrole-3-carbaldehyde.

Annulation of indole via indole radicals: Addition of the 2-indolyl radical to aromatic rings

The reactions of the radicals derived from indoles 4 are described leading to a short synthesis of fused [1,2-a]indoles via radical addition to the benzene ring followed by rearomatisation whilst one example undergoes an unusual radical translocation/addition reaction. (C) 2000 Elsevier Science Ltd.

Thiazolidinedione derivatives, method for preparing the derivatives and pharmaceutical compositions containing same

A thiazolidinedione derivative represented by the following general formula (I): STR1 ?wherein the dotted line represents a single bond or a double bond, the thiazolidinedione ring residue is linked to either of 2-, 3-, 4-, 5- and 6-positions on the indole ring and R represents a group selected from the group consisting of hydrogen atom and alkyl, alkenyl, alkynyl, phenyl, aralkyl, heterocycloalkyl, arylsulfonyl and arylaminocarbonyl groups! or a pharmaceutically acceptable salt thereof exhibits excellent effects of reducing the blood sugar level and of reducing the lipid concentration in blood and is accordingly useful as a therapeutic agent for treating diabates mellitus. These derivatives and pharmaceutically acceptable salt thereof are almost free of any side effect.