71862-34-5

Upstream product

• 85-46-1 1-Naphthalenesulfonyl chloride 
• 74-89-5 methylamine 
• 593-51-1 methylamine hydrochloride 

Downstream Products

• 134133-54-3 N-methyl-N-<3-(4-phenyl-1,2,3,6-tetrahydropyridyl)propyl>-1-naphthalenesulfonamide 
• 1620220-88-3 1,3-dimethyl-1-(tosylmethyl)-1H-benzo[e]indol-2(3H)-one 

Relevant academic research and scientific papers

Antiproliferative activities and SAR studies of substituted anthraquinones and 1,4-naphthoquinones

STAT3 is constitutively active in a large variety of cancers. The search for STAT3 inhibitors led to the discoveries of LLLs 3 and 12, which are substituted anthraquinones. LLL12 is an extremely potent compound that exhibits high levels of antiproliferative activity. Herein the synthesis and evaluation of compounds containing either an anthraquinone or 1,4-naphthoquinone moiety are reported. Analogs were evaluated in several cancer cell lines. Interestingly, it was found that the anthraquinones did not follow the same trends as the 1,4-naphthoquinones in regards to potency. LLL12, which contains a sulfonamide at position 1, was found to be the most potent of the anthraquinones. In contrast, the methyl ketone and methyl ester derivatives (LLLs 3.1 and 5.1) were found to be the most potent of the 1,4-naphthoquinones. Selected 1,4-naphthoquinones were also evaluated in the STAT3 fluorescence polarization assay in order to evaluate their abilities to bind to the STAT3 SH2 domain. They were found to have similar affinities, and their activities suggest that STAT3 is one of their molecular targets.

Compound and medical application thereof in novel coronavirus pneumonia

The invention relates to the field of medicinal chemistry and pharmacotherapeutics, in particular to a compound and medical application of the compound in novel coronavirus pneumonia, and belongs to the technical field of pharmacy. The compound is a compound shown in a formula I or a formula II, or pharmaceutically acceptable salt or ester of the compound. The invention relates to application in preparation of medicines for preventing and/or treating diseases related to novel coronavirus pneumonia.

Compound as well as preparation method and application thereof

The invention relates to the field of medicinal chemistry and pharmacotherapeutics, in particular to a compound as well as a preparation method and an application thereof, and belongs to the technical field of pharmacy, the compound is a compound shown in a formula I or a formula II, or pharmaceutically acceptable salt or ester thereof, and application of the compound in preparation of medicines for preventing and/or treating diseases related to lung cancer.

Compound and medical application thereof in colorectal cancer

The invention relates to the field of medicinal chemistry and pharmacotherapeutics, in particular to a compound and medical application thereof in colorectal cancer, belongs to the technical field of pharmacy, and relates to application in tumor-related activity and the like, in particular to a compound shown in a formula I or a formula II or pharmaceutically acceptable salt or ester thereof, in particular to application in preparation of medicines for preventing and/or treating tumor-related diseases, especially colorectal cancer.

N-Aroylsulfonamide-Photofragmentation (ASAP)-A Versatile Route to Biaryls

The photochemical fragmentation of N-aroylsulfonamides 9 (ASAP) is a powerful method for the preparation of various biaryls. Compounds 9 are easily accessible in two steps from amines by treatment with arenesulfonyl chlorides and aroyl chlorides. Many of these compounds were prepared for the first time. The irradiation takes place in a previously developed continuous-flow reactor using inexpensive UVB or UVC fluorescent lamps. Isocyanates and sulphur dioxide are formed as the only by-products. The ASAP tolerates a variety of functional groups and is even suited for the preparation of phenylnaphthalenes and terphenyls. The ASAP mechanism was elucidated by interaction of photophysical and quantum chemical (DFT) methods and revealed a spirocyclic biradical as key intermediate.

Copper(i)-catalyzed N-H olefination of sulfonamides for: N -sulfonyl enaminone synthesis

This communication reports copper-catalyzed N-H olefination of sulfonamides for enaminone synthesis using saturated ketones as olefin sources. With TEMPO derivatives and O2 as oxidants, this method provided an efficient way to produce various enaminones in good yields. Mechanistic studies helped figure out the stable intermediates and develop novel methodologies for the difunctionalization of saturated ketones.

UV Light Induced Direct Synthesis of Phenanthrene Derivatives from a Linear 3-Aryl-N-(arylsulfonyl) Propiolamides

A novel photochemical approach for the synthesis of phenanthrene derivatives from linear 3-aryl-N-(arylsulfonyl) propiolamides via a tandem radical Smiles rearrangement/C-S bonding/Mallory reaction is disclosed. The control experiment results and isolation of the key intermediates give further insight into the reaction mechanism. Gram scale reaction using a flow reactor demonstrated the synthetic potential applications of our protocol.

Novel arylsulphonamide derivatives and use thereof as therapeutic agents

The present invention relates to novel arylsulphonamide compounds, defined by formula I and the description, as well as their method of preparation and their therapeutic use.