87282-03-9

Upstream product

• 694-59-7 pyridine N-oxide 
• 87281-96-7 3,5-Dimethyl-N-phenyl-benzimidoyl chloride 
• 49764-90-1 3,5-Dimethyl-benzoyl bromide 
• 62-53-3 aniline 
• 6613-44-1 3,5-dimethylbenzoyl chloride 
• 499-06-9 3,5-dimethylbenzoic acid 
• 615-36-1 2-bromoaniline 
• 103-71-9 phenyl isocyanate 
• 611-01-8 2,4-dimethyl-benzoic acid 
• 1227476-15-4 Azobenzene 
• 108-67-8 1,3,5-trimethyl-benzene 
• 201230-82-2 carbon monoxide 
• 172975-69-8 3,5-dimethylphenyl boronic acid 
• 287935-95-9 (3,5-dimethylphenyl)trimethoxysilane 

Relevant academic research and scientific papers

Visible-Light-Promoted Iron-Catalyzed N-Arylation of Dioxazolones with Arylboronic Acids

A visible-light-promoted and simple iron salt-catalyzed N-arylation was achieved efficiently under external photosensitizer-free conditions. Arylboronic acids and bench-stable dioxazolones were used for this cross-coupling reaction. This reaction features high reactivity, wide substrate scope, good functional group tolerance, simple operation procedure, and mild reaction conditions. Preliminary mechanistic investigations were conducted to support a radical pathway. This method may contribute to shift the paradigm of iron-catalyzed C-N bond construction and nitrene transfer chemistry.

Practical one-pot amidation of N -Alloc-, N -Boc-, and N -Cbz protected amines under mild conditions

A facile one-pot synthesis of amides from N-Alloc-, N-Boc-, and N-Cbz-protected amines has been described. The reactions involve the use of isocyanate intermediates, which are generated in situ in the presence of 2-chloropyridine and trifluoromethanesulfonyl anhydride, to react with Grignard reagents to produce the corresponding amides. Using this reaction protocol, a variety of N-Alloc-, N-Boc-, and N-Cbz-protected aliphatic amines and aryl amines were efficiently converted to amides with high yields. This method is highly effective for the synthesis of amides and offers a promising approach for facile amidation.

Synthesis of Amides by Mild Palladium-Catalyzed Aminocarbonylation of Arylsilanes with Amines Enabled by Copper(II) Fluoride

A general Pd-catalyzed synthesis of amides by oxidative aminocarbonylation of arylsilanes under mild conditions was accomplished for the first time. The reaction is promoted by a commercially available copper(II) fluoride, which acts as a dual silane activator and mild oxidant, enabling highly efficient aminocarbonylation of versatile arylsilanes at atmospheric CO pressure. The reaction is tolerant of a wide range of arylsilanes and various sensitive halide functional groups as well as a broad scope of amines are compatible with this oxidative process using cheap CO. A significant aspect involves the increased efficiency by the catalyst system. The reaction represents a segue into the powerful Pd-catalyzed oxidative transformations of organosilanes.

Synthesis of Secondary Amides through the Palladium(II)-Catalyzed Aminocarbonylation of Arylboronic Acids with Amines or Hydrazines and Carbon Dioxide

A new Pd-catalyzed aminocarbonylation of arylboronic acids with amines or phenylhydrazines has been developed. Various secondary amides were produced from readily available substrates and cheap common metal catalysts in a CO atmosphere (balloon). Remarkably, we presents the first example of aminocarbonylations between arylboronic acids and phenylhydrazines.

Peroxide-mediated direct synthesis of amides from aroyl surrogates

An efficient and metal-free method has been developed for the direct synthesis of amides from readily available azobenzenes reacting with aroyl surrogates such as alcohols, methylarenes. A variety of amides were afforded in moderate to good yields through this reaction. It is another example reported by our group for the use of azobenzene as the new radical acceptor.

Interpositus substituted N-aryl benzoyl amines one-step synthesis method of the compound

The invention discloses a one-step synthetic method of meta-substituted N-arylbenzamide compounds. Transition metal ruthenium is used as a catalyst, and the meta-substituted N-arylbenzamide compounds are synthesized in one step through carboxy-based o-C-H functionalization/ decarboxylation coupling reaction of aromatic acid and phenyl isocyanate compounds. The method has the advantages that the raw materials are simple and readily available, the catalyst is cheap, the reaction operation is simple, the utilization rate of atoms is high, the method is environment-friendly and the like.

Ru(II)-catalyzed ortho-amidation and decarboxylation of aromatic acids: A versatile route to meta-substituted N-aryl benzamides

Carboxylate as a promising and valuable directing group has attracted a great deal of attention. However, employing it as a traceless direction group has rarely been reported. We developed the ruthenium-catalyzed amidation of substituted benzoic acids wit

A convenient synthesis of N-aryl benzamides by rhodium-catalyzed ortho-amidation and decarboxylation of benzoic acids

The rhodium-catalyzed amidation of substituted benzoic acids with isocyanates by directed C-H functionalization followed by decarboxylation to afford the corresponding N-aryl benzamides is demonstrated, in which the carboxylate serves as a unique, removable directing group. Notably, less common meta-substituted N-aryl benzamides are generated readily from more accessible paraor ortho-substituted groups by employing this strategy.

Fe-catalysed oxidative C-H functionalization/C-S bond formation

Iron was used as the catalyst for the direct C-H functionalization/C-S bond formation under mild conditions. Various substrates could afford benzothiazoles in moderate to excellent yields. Preliminary mechanistic studies revealed that pyridine played a crucial role for the high yields and selectivities.

Toward optimization of the linker substructure common to transthyretin amyloidogenesis inhibitors using biochemical and structural studies

To develop potent and highly selective transthyretin (TTR) amyloidogenesis inhibitors, it is useful to systematically optimize the three substructural elements that compose a typical TTR kinetic stabilizer: the two aryl rings and the linker joining them. Herein, we evaluated 40 bisaryl molecules based on 10 unique linker substructures to determine how these linkages influence inhibitor potency and selectivity. These linkers connect one unsubstituted aromatic ring to either a 3,5-X2 or a 3,5-X2-4-OH phenyl substructure (X = Br or CH3). Coconsideration of amyloid inhibition and ex vivo plasma TTR binding selectivity data reveal that direct connection of the two aryls or linkage through nonpolar E-olefin or -CH2CH2- substructures generates the most potent and selective TTR amyloidogenesis inhibitors exhibiting minimal undesirable binding to the thyroid hormone nuclear receptor or the COX-1 enzyme. Five high-resolution TTR·inhibitor crystal structures (1.4-1.8 A?) provide insight into why such linkers afford inhibitors with greater potency and selectivity.