3245-95-2

Upstream product

• 13379-98-1 3-[N-(4-methylphenylsulfonyl)amino]propan-1-ol 
• 29281-83-2 4-methylbenzensulphonamide potassium salt 
• 109-64-8 1,3-dibromo-propane 
• 98-59-9 p-toluenesulfonyl chloride 
• 18370-81-5 (3-bromopropyl)amine 
• 70-55-3 toluene-4-sulfonamide 
• 5003-71-4 3-bromopropylamine hydrochloride 

Downstream Products

• 47473-89-2 N-<2-(2-Methoxy-phenoxy)-aethyl>-3-p-toluolsulfonylamino-propylamin 
• 7730-45-2 1-(toluene-4-sulfonyl)azetidine 
• 13379-99-2 N-(3-chloropropyl)-4-methylbenzenesulfonamide 
• 38353-77-4 N-(N³-p-toluenesulfonyl)-3-aminopropylphthalimide 
• 672328-03-9 N-(3-bromopropyl)-N-nitroso-4-methylbenzenesulfonamide 
• 10019-95-1 N-tosylpyrrolidinone 
• 428453-34-3 (Z)-4-methyl-N-(4-phenylbut-3-en-1-yl)benzenesulfonamide 

Relevant academic research and scientific papers

Catalyst-Free Visible-Light-Mediated Iodoamination of Olefins and Synthetic Applications

Herein we report a catalyst- and metal-free visible-light-mediated protocol enabling the iodoamination of miscellaneous olefins. This protocol is characterized by high yields under environmentally benign reaction conditions utilizing commercially available substrates and a green and biodegradable solvent. Furthermore, the protocol allows for late-stage functionalization of bioactive molecules and can be scaled to gram quantities of product, which offers manifold possibilities for further transformations, including morpholine, piperidine, pyrrolidine, and aziridine synthesis.

An endoplasmic reticulum-targeted organic photothermal agent for enhanced cancer therapy

Developing selectively targeted photothermal agents to reduce side effects in photothermal therapy remains a great challenge. Inspired by the key role of endoplasmic reticulum in the protein synthesis and intracellular signal transduction, particularly for the immunogenic cell death induced by endoplasmic reticulum stress, we developed an endoplasmic reticulum-targeted organic photothermal agent (Ts-PT-RGD) for enhancing photothermal therapy of tumor. The photothermal agent was covalently attached with 4-methylbenzenesulfonamide and cyclic Arg-Gly-Asp (cRGD) peptide for realizing the targeting of endoplasmic reticulum and tumor cell. Owing to its amphiphilic properties, it readily self-assembles in water to form nanoparticles. The photothermal agent possesses excellent photophysical properties and biological compatibility. In vitro and in vivo experiments demonstrate that it can actively target endoplasmic reticulum and effectively ablate tumor with near-infrared laser.

Efficient N-acylation of sulfonamides using cesium salt of Wells–Dawson heteropolyacid as catalyst: Synthesis of new N-acyl sulfonamides and cyclic imides

N-acylation of substituted sulfonamides with different anhydrides in the presence of Cesium salt of Wells–Dawson heteropolyacid (Cs5HP2W18O62) as an efficient and reusable catalyst was investigated for the first time. ?Cs5HP2W18O62 was used with a catalytic amount in water as a green solvent. At room temperature, a series of N-acylsulfonamides were synthesized, while under refluxing conditions, new cyclic imides containing sulfonyl group were obtained. Atom-economy, high yields, easy work-up, as well as simple catalyst recovery and reusability are the key features of this procedure.

In silico identification, design and synthesis of novel piperazine-based antiviral agents targeting the hepatitis C virus helicase

A structure-based virtual screening of commercial compounds was carried out on the HCV NS3 helicase structure, with the aim to identify novel inhibitors of HCV replication. Among a selection of 13 commercial structures, one compound was found to inhibit the subgenomic HCV replicon in the low micromolar range. Different series of new piperazine-based analogues were designed and synthesised, and among them, several novel structures exhibited antiviral activity in the HCV replicon assay. Some of the new compounds were also found to inhibit HCV NS3 helicase function in?vitro, and one directly bound NS3 with a dissociation constant of 570?±?270?nM.

Syntheses of novel N-([ 18F]fluoroalkyl)-N-nitroso-4-methyl-benzenesulfonamides and decomposition studies of corresponding 19F- and bromoanalogues: Potential new compounds for the 18F-labelling of radiopharmaceuticals

N-([18F]fluoroalkyl)-N-nitroso-4-methyl-benzensulfonamides [n-alkyl = (-CH2) [18,19F]F, n = 2-4)] were synthesized in radiochemical yields ranging from 75-90% to provide new secondary labelling precursors for the syntheses

Design and Synthesis of Macromonocyclic Polyamines Composed of Natural Methylene Arrays

A general synthetic method applicable to acyclic and cyclic polyamines was developed.The methodology was exemplified by systematical synthesis of twelve macromonocyclic polyamines, 1 (N4) through 12 (N8), composed of the combination of four natural polyamine segments, spermidine, spermine, thermine, and thermospermine.These twelve designed macrocycles are exhausted numbers of possible structures defined by three arbitrarily chosen criteria concerning with methylene chain arrays and nitrogen content (four to eight).The common elements of the structural characteristics were analyzed and were found to be reduced to readily available three classes of simple N,N'-ditosylalkanediamines derived from diamines and triamine.Nitrogen content was increased systematically through the reaction of N,N'-ditosylalkanediamine with one of three ω-phthalimidated electrophiles followed by regeneration of the same functionality at symmetrical both terminals as the starting materials via a series of transformation reaction, in excellent yields.Tractable formamide intermediate profits the facile synthesis of acyclic polyamines with long chains.Cyclization was achieved, under high dilution conditions, through the reaction of α,ω-bis(tosylamide) with α,ω-ditosylates in DMF in the presence of cesium carbonate.The cyclization occurred in practical synthetic yields even in the formation of multi-membered ring when the shorter electrophile and the longest α,ω-bis(tosylamide) reacted.

Ring-closure Reactions. Part 23. Kinetics of Formation of Three- to Seven-membered-ring N-Tosylazacycloalkanes. The Role of Ring Strain in Small- and Common-sized-ring Formation

Rates of cyclisation of a series of anions derived from N-tosyl-ω-bromoalkylamines to nitrogen heterocycles with three to seven members in Me2SO-H2O (99:1) have been studied.Rates vary markedly with ring size in the order 5 > 3 > 6 > 7 ca. 4.First order rate constants for cyclisation have been translated into effective molarities (EM) with reference to an appropriate intermolecular model reaction.Comparison of the present results with available literature data on SN2 ring-closure reactions leading to small- and common-sized rings reveals that the ease of formation of three-membered rings is much more structure-dependent than that of the higher homologues.This remarkable behaviour is believed to parallel the unique way in which the stability of three-membered rings is affected by structure.As a rule, the ease of cyclisation appears to bear an inverted relationship to the assumed strain energy of the ring product.The apparent opposition of this rule to earlier conclusions in the literature is discussed.