81344-98-1

Upstream product

• 1190709-21-7 C₂₂H₁₉NO₄S 
• 100-66-3 methoxybenzene 
• 7507-86-0 2-bromo-5-methoxy-benzaldehyde 
• 1006-94-6 5-methoxylindole 
• 120-72-9 indole 
• 104-92-7 1-bromo-4-methoxy-benzene 
• 1027787-52-5 C₂₃H₂₁NO₄S 
• 6037-74-7 2-p-anisidino-1-(4-methoxy-phenyl)-ethanone 

Relevant academic research and scientific papers

Synthesis and antimycobacterial activity of 3-phenyl-1h-indoles

Tuberculosis has been described as a global health crisis since the 1990s, with an estimated 1.4 million deaths in the last year. Herein, a series of 20 1H-indoles were synthesized and evaluated as in vitro inhibitors of Mycobacterium tuberculosis (Mtb) g

Synthesis of 3-arylindole derivatives from nitroalkane precursors

3-Arylindole derivatives were synthesized by Cu(i) catalysed intramolecular Ullmann coupling of 2-bromoarylaminoalkanes. 2-Bromoarylaminoalkanes were synthesized from 2-bromoarylnitroalkanes, which in turn prepared through AlCl3-mediated Friede

Metal-free direct arylations of indoles and pyrroles with diaryliodonium salts

Chemical equations presented. Direct arylations of indoles and pyrroles with differently substituted diaryliodonium salts were shown to efficiently proceed in the absence of metal catalysts.

The synthesis of 2- and 3-aryl indoles and 1,3,4,5-tetrahydropyrano[4,3-b]indoles and their antibacterial and antifungal activity

A series of 2- and 3-aryl substituted indoles and two 1,3,4,5-tetrahydropyrano[4,3-b]indoles were synthesized from indole and 5-methoxyindole. The 2-aryl indoles were synthesized from the 1-(phenylsulfonyl)indole derivatives using magnesiation followed by iodination. The 2-iodinated compounds were then subjected to Suzuki-Miyaura reactions. In addition, the 3-aryl indoles were made from the corresponding 3-bromoindoles using Suzuki-Miyaura reactions. The 1,3,4,5-tetrahydropyrano[4,3-b]indoles were also synthesized from 1-(phenylsulfonyl)indole by magnesiation followed by treatment with allylbromide. The product was then converted into [2-allyl-1-(phenylsulfonyl)-1H-indol-3-yl]methanol which upon exposure to Hg(OAc)2 and NaBH4 afforded tetrahydropyrano[4,3-b]indoles. A number of the 2- and 3-aryl indoles displayed noteworthy antimicrobial activity, with compound 13a displaying the most significant activity (3.9 μg/mL) against the Gram-positive micro-organism Bacillus cereus.

Direct palladium-catalyzed C-3 arylation of free (NH)-indoles with aryl bromides under ligandless conditions

(Chemical Equation Presented) A new method for the efficient, practical, and highly regioselective direct palladium-catalyzed C-3 arylation of free (NH)-indole and its electron-rich 1-unsubstituted derivatives under ligandless conditions is described. The reactions, which are run outside a glovebox without purification of solvent and reagents, involve treatment of free (NH)-indoles with activated, unactivated, and deactivated aryl bromides in refluxing toluene in the presence of K2CO3 as the base and a catalyst system consisting of a combination of Pd(OAc)2 and benzyl(tributyl)ammonium chloride. The experimental results are consistent with a catalytic cycle based on an electrophilic palladation pathway at the 3-position of 1-indolyl potassium salts.

COMPOUNDS AND METHODS FOR TREATING PROTEIN FOLDING DISORDERS

The invention is directed to compounds and methods for treating protein folder disorders. In certain embodiments the invention provides compounds and methods for treating neurodegenerative diseases such as Alzheimer's disease, tauopathy, cerebral amyloid angiopathy, Lewy body disease, dementia, Huntington's disease and prion-based spongiform encelopathy. The invention further provides compounds, methods and pharmaceutical compositions for inhibiting tau protein, Aβ protein or α-synuclein protein aggregation.