5873-12-1

Upstream product

• 302-84-1 serin 
• 98-59-9 p-toluenesulfonyl chloride 
• 56-45-1 L-serin 
• 312-84-5 D-Serine 
• 308245-98-9 (R)-N-[1'-(2-Furyl)-2'-benzyloxyethyl]-N-[2-(p-tolylsulfonyloxy)ethyl]toluene-p-sulfonamide 
• 308246-08-4 (R)-N-[1'-(2-Furyl)-2'-benzyloxyethyl]-N-(2-phenylselenoethyl)toluene-p-sulfonamide 
• 219715-78-3 (R)-N-[1'-(2-Furyl)-2'-benzyloxyethyl]toluene-p-sulfonamide 
• 5873-11-0 3-hydroxy-2-{(4-methylphenyl)sulphonamino}propanoic acid 

Downstream Products

• 7663-92-5 N-tosyl-L-serine 
• 5873-13-2 (R)-2-(p-Tolylsulfonamido)serine 
• 17136-46-8 N-tosyl-D-serine methyl ester 
• 21752-11-4 N-(toluene-4-sulfonyl)-D-serine hydrazide 
• 304460-78-4 N-(1-hydroxybutan-2-yl)-4-methylbenzenesulfonamide 
• 91958-80-4 (S)-4-acetoxymethyl-3-(toluene-4-sulfonyl)-oxazolidin-5-one 

Relevant academic research and scientific papers

Synthesis and Structure-Activity Relationships of Arylsulfonamides as AIMP2-DX2 Inhibitors for the Development of a Novel Anticancer Therapy

AIMP2-DX2, a splicing variant of AIMP2, is up-regulated in lung cancer, possesses oncogenic activity, and results in tumorigenesis. Specifically inhibiting the interaction between AIMP2-DX2 and HSP70 to suppress AIMP2-DX2-dependent cancers with small molecules is considered a promising avenue for cancer therapeutics. Optimization of hit BC-DXI-04 (IC50 = 40.1 μM) provided new potent sulfonamide based AIMP2-DX2 inhibitors. Among these, BC-DXI-843 showed improved inhibition against AIMP2-DX2 (IC50 = 0.92 μM) with more than 100-fold selectivity over AIMP2 in a luciferase assay. Several binding assays indicated that this compound effectively induces cancer cell apoptosis by specifically interrupting the interaction between DX2 and HSP70, which leads to the degradation of DX2 via Siah1-mediated ubiquitination. More importantly, BC-DXI-843 demonstrated in vivo efficacy in a tumor xenograft mouse model (H460 cells) at a dosage of 50 mg/kg, suggesting it as a promising lead for development of novel therapeutics targeting AIMP2-DX2 in lung cancer.

Synthesis, molecular docking and pharmacological investigation of some 4-methylphenylsulphamoyl carboxylic acid analogs

Compounds bearing sulphonyl and amino acid moieties are considered the basis for sulfa drug development. The synthesis of 4-methylphenylsulphamoyl carboxylic acids and the evaluation of their pharmacological activities are reported. The synthesis of these

Iodine-Catalyzed Synthesis of Chiral 4-Imidazolidinones Using α-Amino Acid Derivatives via Dehydrogenative N-H/C(sp3)-H Coupling

An efficient method for the asymmetric synthesis of 4-imidazolidinones via an iodine-catalyzed intramolecular N-H/C(sp3)-H activation of readily available and abundant feedstocks, amino acids, and amines is described. The reaction proceeded under visible light irradiation to afford a variety of 4-imidazolidinone derivatives under mild conditions in moderate to excellent yields. Secondary and tertiary C(sp3)-H bonds were aminated, and various functional groups were tolerated.

New carboxamides bearing benzenesulphonamides: Synthesis, molecular docking and pharmacological properties

Ten new derivatives of benzenesulphonamide bearing carboxamide functionality were synthesized and investigated for their in vitro antimicrobial, antioxidant and in vivo anti-inflammatory activities. Compound 9d inhibited carrageenan induced rat-paw oedema

Pd(II)-Catalyzed Aminofluorination of Alkenes in Total Synthesis 6-(R)-Fluoroswainsonine and 5-(R)-Fluorofebrifugine

The total syntheses of two fluorinated alkaloids, 6-(R)-fluoroswainsonine and 5-(R)-fluorofebrifugine, are described. Both encompass (4aS,7R,8aR)-7-fluoro-5-tosylhexahydro-4H-[1,3]dioxino[5,4-b]pyridine as a key synthon which is obtained through a further

Pd(II)-Catalyzed Aminofluorination of Alkenes in Total Synthesis 6-(R)-Fluoroswainsonine and 5-(R)-Fluorofebrifugine

The total syntheses of two fluorinated alkaloids, 6-(R)-fluoroswainsonine and 5-(R)-fluorofebrifugine, are described. Both encompass (4aS,7R,8aR)-7-fluoro-5-tosylhexahydro-4H-[1,3]dioxino[5,4-b]pyridine as a key synthon which is obtained through a further

Palladium-Catalyzed Modular Synthesis of Substituted Piperazines and Related Nitrogen Heterocycles

We report here a novel method for the modular synthesis of highly substituted piperazines and related bis-nitrogen heterocycles via a palladium-catalyzed cyclization reaction. The process couples two of the carbons of a propargyl unit with various diamine components to provide nitrogen heterocycles in generally good to excellent yields and high regio- and stereochemical control. (Chemical Equation Presented).

Palladium(II) mixed-ligand complexes containing 2,2′-bipyridine derivatives and 4-toluenesulfonyl-l-serine: Synthesis, characterization, and crystal structure determination

The 4-toluenesulfonyl-L-serine ligand (1), (tsserH2), was prepared from the reaction of L-serine and 4-toluenesulfonyl chloride in sodium hydroxide solution 1 M. The complexes [Pd(4,4′-dmbipy)(tsser)] (2) and [Pd(5,5′-dmbipy)(tsser)].0.5CH

The effect of hydrogen bond on Br?nsted acid-catalyzed intramolecular hydroamination of unfunctionalized olefins

The catalytic activity of benzoic acid could be increased by introducing a hydrogen bond donor group at the ortho-position. Preliminary DFT calculation indicated that the activation of CC double bond was realized by the action of both the carboxyl group and the hydrogen bond donor. The amino group was brought to the activated CC bond by the interaction between the carboxyl oxygen and amino proton. This interaction also increased the nucleophilicity of the amino group. Thus, in the presence of 20 mol % of 2-(trifluoromethanesulfonamido)benzoic acid, intramolecular hydroamination of unfunctionalized olefins gave the corresponding products in up to 95% isolated yields.

Development of amino acid conjugated sulfonamides as potent antiulcer agent

A series of 2-{[(4-methylphenyl) sulfonyl] amino}-3-sulfanylpropanoic acid (1a) and its analogs 1b-j have been synthesized. These compounds were screened for their in vivo efficacy in pyloric ligation model. Compounds 1a and 1b with higher antiulcer potential were further screened in other gastric models to explore the mode of antiulcer action. To further understand the mode of action, in vitro inhibition of H+/K+ ATPase activity in gastric microsome isolated from rat stomach was studied. This was rationalized by in silico experiments.