90481-72-4

Upstream product

• 52488-36-5 4-bromo-1H-indole 
• 98-59-9 p-toluenesulfonyl chloride 
• 90481-71-3 N-tosyl-3-bromo-2-ethenylaniline 
• 90481-67-7 (2-Bromo-6-nitro-benzyl)-triphenyl-phosphonium; bromide 
• 58579-54-7 3-bromo-2-(bromomethyl)-1-nitrobenzene 
• 95969-07-6 5-chloro-4-oxo-N-(p-toluenesulfonyl)-4,5,6,7-tetrahydroindole 
• 81038-31-5 1-tosyl-1H-indol-4-amine 
• 90481-68-8 1-bromo-2-ethenyl-3-nitrobenzene 
• 90481-69-9 3-bromo-2-ethenylaniline 
• 603-83-8 3-nitro-o-tolylamine 
• 55289-35-5 2-bromo-6-nitrotoluene 

Downstream Products

• 90481-75-7 4-(2-phenylethen-1-yl)-1-tosylindole 
• 90481-76-8 4-(2-phthalimidoethen-1-yl)-1-tosylindole 
• 130131-64-5 methyl (2Z)-2-(acetylamino)-3-(1-tosyl-1H-indol-4-yl)prop-2-enoate 
• 90481-85-9 (Z)-2-Acetylamino-3-[4-bromo-1-(toluene-4-sulfonyl)-1H-indol-3-yl]-acrylic acid methyl ester 
• 90481-73-5 (E)-methyl 3-(1-tosyl-1H-indol-4-yl)acrylate 
• 108868-37-7 4-bromo-3-(2-acetamido-2-carbomethoxyethen-1-yl)-1-tosylindole 
• 162893-61-0 (Z)-3-[4-Bromo-1-(toluene-4-sulfonyl)-1H-indol-3-yl]-2-tert-butoxycarbonylamino-acrylic acid methyl ester 
• 122145-35-1 4-(2-carbethoxyprop-2-enyl)-1-tosylindole 
• 31271-90-6 1-(p-toluenesulfonyl)-1H-indole 
• 1258408-28-4 benzyl 4-(toluene-4-sulfonyl)-4,6,6a,7,9,10-hexahydro-4,8,10a-triaza-acephenanthrylene-8-carboxylate 
• 84807-08-9 benzyl 4-(1H-indol-4-yl)-piperazine-1-carboxylate 
• 1258408-24-0 benzyl 4-(3-formyl-1H-indol-4-yl)-piperazine-1-carboxylate 
• 1258408-26-2 benzyl 4-[3-formyl-1-(toluene-4-sulfonyl)-1H-indol-4-yl]-piperazine-1-carboxylate 
• 88299-06-3 (E)-2-methyl-4-(1-tosyl-1H-indol-4-yl)but-3-en-2-ol 

Relevant academic research and scientific papers

The total synthesis of (?)-indolactam I

The first total synthesis of (?)-indolactam I (1) is reported. An efficient synthetic route was established to furnish the natural product in 8 steps. This strategy employed a copper-catalyzed amino acid arylation, peptide coupling, and Lewis acid-mediate

COMPOUNDS AND USES THEREOF

The present disclosure features compounds useful for the treatment of BAF complex-related disorders.

Rhodium(II)-Catalyzed [4+3] Cyclization of Triazoles with Indole Derivatives and Its Application in the Total Synthesis of (±)-Aurantioclavine

An efficient rhodium(II)-catalyzed [4+3] cyclization reaction of 1-sulfonyl-1,2-3-triazoles and indoles was developed. Azepino[5,4,3- cd]indoles, which are widely distributed in ergot alkaloids with various biological activities, could be obtained in good

Iodine-Mediated Electrochemical C(sp2)-H Amination: Switchable Synthesis of Indolines and Indoles

A metal-free electrochemical intramolecular C(sp2)-H amination using iodine as a mediator was developed. This method enables a switchable synthesis of indoline and indole derivatives, respectively, from easily available 2-vinyl anilines.

The Synthesis and Biological Evaluation of Indolactam Alkaloids

In this work, we execute a general synthetic strategy to access novel indolactam alkaloids, which are agonists of protein kinase C. This protocol allowed for the most efficient reported syntheses of indolactam V (ILV) stereoisomers, while also affording t

ISOXAZOLE DERIVATIVE AS MUTATED ISOCITRATE DEHYDROGENASE 1 INHIBITOR

It has been found that a compound of the general formula (I) having an isoxazole skeleton has excellent inhibitory activity against mutant IDH1 protein and inhibits the production of 2-HG by this protein, while the compound is also capable of effectively inhibiting the growth of various tumors expressing the protein. In the formula, R1, R2, R3, Y, and Z are as defined in claim 1.

Modular Total Synthesis of Protein Kinase C Activator (-)-Indolactam v

A concise, eight-step total synthesis of (-)-indolactam V, a nanomolar agonist of protein kinase C, is reported. The synthesis relies upon an efficient copper-catalyzed amino acid arylation to establish the indole C4-nitrogen bond. This cross-coupling met

Preparation of No-Carrier-Added 6-[18F]Fluoro-l-tryptophan via Cu-Mediated Radiofluorination

18F-Labeled aromatic amino acids exhibit great potential for diagnostic applications using positron emission tomography. However, the introduction of18F into aromatic compounds remains challenging, and novel fluorination methods facilitating easy access to18F-labeled arenes are highly sought after. In recent years, novel metal-mediated fluorination methods have been reported and transferred into radiochemistry. Based on Cu-mediated radiofluorination, a two-step synthesis of no-carrier-added (n.c.a.) 6-[18F]fluoro-l-tryptophan was developed. 6-[18F]Fluoro-l-tryptophan was synthesized with an overall radochemical yield of 16 ± 4% within 110 min and a specific activity of 280 GBq μmol–1. The radiochemical purity was more than 99 %. The developed method allowed access to radiofluorinated tryptophan derivatives in high radiochemical yields and opens new ways to provide radiofluorinated amino acids. Furthermore, the reaction conditions were optimized to facilitate automation.

Room-Temperature Gold-Catalysed Arylation of Heteroarenes: Complementarity to Palladium Catalysis

Tailoring of the pre-catalyst, the oxidant and the arylsilane enables the first room-temperature, gold-catalysed, innate C?H arylation of heteroarenes. Regioselectivity is consistently high and, in some cases, distinct from that reported with palladium ca

Novel Aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands.

By introducing distal substituents on a tetracyclic scaffold resembling the ergoline structure, two series of analogues were achieved exhibiting subnanomolar receptor binding affinities for the dopamine D2 and serotonin 5-HT6 receptor subtype, respectively. While the 5-HT 6 ligands were antagonists, the D2 ligands displayed intrinsic activities ranging from full agonism to partial agonism with low intrinsic activity. These structures could potentially be interesting for treatment of neurological diseases such as schizophrenia, Parkinson's disease, and cognitive deficits.