243844-35-1

Upstream product

• 17849-38-6 2-Chlorobenzyl alcohol 
• 98-59-9 p-toluenesulfonyl chloride 
• 118-92-3 anthranilic acid 
• 5344-90-1 2-Aminobenzyl alcohol 
• 90312-02-0 N-(2-hydroxymethylphenyl)-4-methylbenzenesulfonamide 

Downstream Products

• 177763-21-2 4-methyl-N-[2-(3-methyl-but-2-enyl)-phenyl]-benzenesulfonamide 
• 1176941-84-6 C₁₉H₂₃NO₃S 
• 1269261-63-3 2-(bromomethyl)-1-(toluene-4-sulfonyl)-1,2,3,4-tetrahydroquinoline 
• 1394978-77-8 C₂₇H₂₆N₂O₅S 

Relevant academic research and scientific papers

A [4+3] Cycloaddition Reaction of Aza-ortho-quinone Methides with C,N-Cyclic Azomethine Imines for Synthesis of 1,2,4-Triazepines

The base-induced formal [4+3] cycloaddition reaction of C,N-cyclic azomethine imines with aza-ortho-quinone methides, generated in situ, is reported. This protocol provided an efficient method for the synthesis of biologically important 1,2,4-triazepine derivatives, with a wide substrate scope and excellent functional-group tolerance, and it gives moderate to excellent yields under mild conditions. Several of the derivatives exhibited in vitro antitumor activities against the A2780 cell line in a screening of the cancer cell lines HCT-116, H2228, and A2780 by an MTT assay.

Benzoazacyclo compound and application thereof

The invention discloses a compound represented by a formula (I) or a salt thereof. The invention further provides an application of the compound represented by the formula (I) or the salt thereof in preparation of drugs for preventing or treating hepatic fibrosis diseases. The invention provides a new benzoazacyclo compound or a salt thereof, and it is found that the benzoazacyclo compound has anobvious anti-hepatic fibrosis effect for the first time, and thus a new application of the benzoazacyclo compound in preparation of drugs for preventing hepatic fibrosis diseases or treating hepatic fibrosis diseases is found out.

An Effective Method for the Synthesis of 1,3-Dihydro-2H-indazoles via N-N Bond Formation

The [4+1] cycloaddition reaction of bifunctional amino reagents has been achieved with in situ formed aza-ortho-quinone methides. Specifically, N-(tosyloxy)carbamates were used as an N1 synthon and bifunctional amino reagents for this transformation, which provides a metal-free, catalyst-free, and oxidant-free strategy to form nitrogen-nitrogen bonds. (Figure presented.).

A [4 + 3] Annulation Reaction of aza- o-Quinone Methides with Arylcarbohydrazonoyl Chlorides for Synthesis of 2,3-Dihydro-1 H-benzo[ e][1,2,4]triazepines

An unprecedented [4 + 3] annulation reaction of aza-ortho-quinone methides with arylcarbohydrazonoyl chlorides has been achieved under mild conditions. The annulation underwent a sequential conjugate addition/intramolecular annulation/rearrangement, providing a useful method for the synthesis of biologically interesting 2,3-dihydro-1H-benzo[e][1,2,4]triazepine.

Palladium(II)-catalyzed aerobic intramolecular allylic C[sbnd]H activation for the synthesis of indolines

A method for the preparation of indolines via palladium-catalyzed aerobic intramolecular allylic C[sbnd]H activation was developed. Oxygen was successfully used as oxidant with catalytic amount of 1,4-benzoquinone. 16 examples were reported, the majority of substrates gave moderate to good yields.

Pd(II)-catalyzed enantioselective intramolecular oxidative amination utilizing (+)-camphorsulfonic acid

An enantioselective Pd(II)-catalyzed intramolecular oxidative amination reaction was developed utilizing the commercially available chiral X-type ligand (1S)-(+)-camphorsulfonic acid. The Wacker-type cyclization produced chiral indoline products with enantioselectivies up to 45% ee. Electronic structure calculations employing density functional theory support a trans-aminopalladation mechanism.

Tandem [3 + 2] cycloaddition/1,4-addition reaction of azomethine ylides and aza-o-quinone methides for asymmetric synthesis of imidazolines

An enantioselective synthesis of biologically important imidazolidines has been achieved via a tandem [3 + 2] cycloaddition/1,4-addition reaction of azomethine ylide and aza-o-quinone methides. With the use of this tool, various imidazolidine derivatives are obtained in good yields with excellent diastereoselectivities and enantioselectivities.

A Pd(II)-catalyzed oxidative cyclization for the preparation of aryl-fused six-membered nitrogen heterocycles with 2-acetoxy functionality

A Pd(II)-catalyzed oxidative cyclization of olefinic tosylamides was developed for the preparation of aryl-fused and N-containing six-membered heterocycles. Under optimized conditions the reaction proceeded with high activity and selectivity, with yields

Transition-metal-free approach to synthesis of indolines from N-(ortho-chloromethyl)aryl amides and iodonium ylides

A transition-metal-free method for the synthesis of indolines has been developed. In the presence of K2CO3, the cyclization reaction of N-(ortho-chloromethyl)aryl amides and iodonium ylides proceeded smoothly at room temperature in moderate to good yields.

Synthesis of indoles through highly efficient cascade reactions of sulfur ylides and N-(ortho-chloromethyl)aryl amides

Batting the ylides: A simple procedure carried out under mild conditions allows the direct and efficient synthesis of structurally diverse indoles. This approach involves a cascade reaction of sulfur ylides and N-(ortho-chloromethyl) aryl amides (see scheme). Copyright