71947-05-2

Upstream product

• 31614-66-1 tributyl(p-tolyl)stannane 
• 17201-43-3 4-cyanobenzyl bromide 
• 623-00-7 4-bromobenzenecarbonitrile 
• 104-82-5 4-Methylbenzyl chloride 
• 696-61-7 4-tolylmagnesium chloride 
• 15106-88-4 di(p-tolyl)zinc 
• 5142-75-6 tri(p-tolyl)bismuth 
• 874-88-4 4-(iodomethyl)benzonitrile 
• 5720-05-8 4-methylphenylboronic acid 
• 874-86-2 4-cyanobenzyl chloride 
• 623-26-7 terephthalonitrile 
• 126747-14-6 4-cyanophenylboronic acid 
• 589-18-4 4-Methylbenzyl alcohol 
• 106-42-3 para-xylene 

Relevant academic research and scientific papers

Method for synthesizing diaryl methane derivative

The invention aims to provide a method for synthesizing a diaryl methane derivative. The method is characterized in that tris (dibenzylideneacetone) dipalladium is used as a catalyst, an organic antimony compound is used as a nucleophilic reagent, benzyl bromide and benzyl chloride are used as electrophilic reagents, toluene is used as a solvent, and the diaryl methane derivative is synthesized through direct cross coupling under the air atmosphere condition. The method has the characteristics of good substrate universality, good functional group tolerance, simplicity and convenience in operation and the like.

Palladium-Catalyzed Hiyama Coupling of Benzylic Ammonium Salts via C-N Bond Cleavage

The first palladium-catalyzed Hiyama cross-coupling of arylsilanes with benzyltrimethylammonium salts is reported. The reaction proceeds smoothly to facilitate C(sp2)-C(sp3) bond formation via cleavage of the C-N bond and provides a useful approach to various diarylmethanes with a broad substrate scope and excellent functional group tolerance in good to excellent yields.

Dual copper- and photoredox-catalysed C(sp2)-C(sp3) coupling

The use of copper catalysis with visible light photoredox catalysis in a cooperative fashion has recently emerged as a versatile means of developing new C-C bond forming reactions. In this work, dual copper and photoredox catalysis is exploited to effect C(sp2)-C(sp3) cross-couplings between aryl boronic acids and benzyl bromides.

The Dual Role of Benzophenone in Visible-Light/Nickel Photoredox-Catalyzed C?H Arylations: Hydrogen-Atom Transfer and Energy Transfer

A dual catalytic protocol for the direct arylation of non-activated C(sp3)?H bonds has been developed. Upon photochemical excitation, the excited triplet state of a diaryl ketone photosensitizer abstracts a hydrogen atom from an aliphatic C?H bond. This inherent reactivity was exploited for the generation of benzylic radicals which subsequently enter a nickel catalytic cycle, accomplishing the benzylic arylation.

A SO2F2 mediated mild, practical, and gram-scale dehydroxylative transforming primary alcohols to quaternary ammonium salts

A simple, practical and gram-scale process for direct transformation of primary alcohols or silyl ethers to ammonium salts was developed. This method has the feathers of easy work-up (a simple filtration), mild condition, high yield, great practicality and robustness. And the application of the ammonium salts in Suzuki coupling reaction was also accomplished.

Construction of Di(hetero)arylmethanes Through Pd-Catalyzed Direct Dehydroxylative Cross-Coupling of Benzylic Alcohols and Aryl Boronic Acids Mediated by Sulfuryl Fluoride (SO2F2)

A practical Pd-catalyzed direct dehydroxylative coupling of (hetero)benzylic alcohols with (hetero)arylboronic acids for the constructions of di(hetero)arylmethane derivatives under SO2F2 was described. This new method provided a strategically distinct approach to di(hetero)arylmethane derivatives from readily available and abundant benzylic alcohols under mild condition.

Structure-Activity Relationship Studies of Tolfenpyrad Reveal Subnanomolar Inhibitors of Haemonchus contortus Development

Recently, we have discovered that the registered pesticide, tolfenpyrad, unexpectedly and potently inhibits the development of the L4 larval stage of the parasitic nematode Haemonchus contortus with an IC50 value of 0.03 μM while displaying good selectivity, with an IC50 of 37.9 μM for cytotoxicity. As a promising molecular template for medicinal chemistry optimization, we undertook anthelmintic structure-activity relationships for this chemical. Modifications of the left-hand side (LHS), right-hand side (RHS), and middle section of the scaffold were explored to produce a set of 57 analogues. Analogues 25, 29, and 33 were shown to be the most potent compounds of the series, with IC50 values at a subnanomolar level of potency against the chemotherapeutically relevant fourth larval (L4) stage of H. contortus. Selected compounds from the series also showed promising activity against a panel of other different parasitic nematodes, such as hookworms and whipworms.

Palladium catalyzed Suzuki cross-coupling of benzyltrimethylammonium salts via C-N bond cleavage

A palladium catalyzed Suzuki cross-coupling for construction of Csp3-Csp2 bond via Csp3-N bond activation of benzyltrimethyl-ammonium salt is described. This reaction not only offered a highly efficient approach to diarylmethanes but also paved the way for the application of benzyltrimethylammonium salts in the palladium catalyzed cross coupling reactions.

Visible-Light-Mediated Aromatic Substitution Reactions of Cyanoarenes with 4-Alkyl-1,4-dihydropyridines through Double Carbon-Carbon Bond Cleavage

Novel aromatic substitution reactions of cyanoarenes with 4-alkyl-1,4-dihydropyridines as alkylating reagents in the presence of a catalytic amount of a photoredox catalyst proceed smoothly to give the corresponding alkyl-substituted arenes in good to high yields. The present reaction system realizes a novel C-C bond-forming reaction between two fragments generated from the C-C bond-cleavage reactions of two independent substrates.

Efficient synthesis of diarylmethane derivatives by PdCl2 catalyzed cross-coupling reactions of benzyl chlorides with aryl boronic acids in aqueous medium

The research provides a simple and efficient method for preparing diarylmethane derivatives using the cross-coupling reaction of benzyl chlorides and aryl boronic acids catalyzed by palladium chloride in DMF aqueous solution without additional ligand.