53364-99-1

Upstream product

• 109-76-2 Trimethylenediamine 
• 98-59-9 p-toluenesulfonyl chloride 
• 98-88-4 benzoyl chloride 
• 100-52-7 benzaldehyde 
• 109-64-8 1,3-dibromo-propane 
• 18522-92-4 sodium p-toluenesulfonamide 

Downstream Products

• 60147-27-5 10,14-bis-(toluene-4-sulfonyl)-1,4,7-trioxa-10,14-diaza-cyclohexadecane 
• 99998-90-0 N,N'-(propane-1,3-diyl)bis(N,4-dimethylbenzenesulfonamide) 
• 35980-65-5 1,4,7-tri(p-toluenesulfonyl)-1,4,7-triazacyclodecane 
• 126544-44-3 (Z)-1,5-Bis-(toluene-4-sulfonyl)-2,3,4,5,6,9-hexahydro-1H-[1,5]diazonine 
• 35980-67-7 1,5,9-tritosyl-1,5,9-triazacyclododecane 
• 152488-72-7 C₂₅H₃₈N₂O₈S₂ 
• 87265-92-7 N,N'-bis(tosyl)-N,N'-bis(2-cyanoethyl)-1,3-diaminopropane 
• 115368-15-5 N-(2-hydroxyethyl)-4-methyl-N-(3-((4-methylphenyl)sulfonamido)propyl)benzenesulfonamide 
• 111280-66-1 Methanesulfonic acid 2-[{3-[(2-methanesulfonyloxy-ethyl)-(toluene-4-sulfonyl)-amino]-propyl}-(toluene-4-sulfonyl)-amino]-ethyl ester 
• 121821-31-6 N,N'-bis(3-phthalimidopropyl)-N,N'-ditosyl-1,3-propanediamine 
• 121821-30-5 N,N'-bis(4-phthalimidobutyl)-N,N'-ditosyl-1,3-propanediamine 
• 60147-25-3 4-oxa-1,7-bis(p-toluenesulphonyl)-1,7-diazacyclodecane 
• 176107-53-2 N,N'-bis(p-toluenesulfonamido)-N-(tert-butoxycarbonyl)-1,3-propanediamine 
• 16077-33-1 1,3-ditosylhexahydro-1,3-diazine 

Relevant academic research and scientific papers

Method for preparing diazacyclooctane intermediate and diazacyclooctane

The invention provides a method for preparing a diazacyclooctane intermediate and diazacyclooctane. The preparation method comprises the following steps: synthesizing 1,5-bis(p-toluenesulfonyl)-1,5-diazacyclooctane from 1,3-bis(p-toluenesulfonyl)-1,3-dioxypropane, 1,3-bis(p-toluenesulfonyl)-1,3-propane diamine and sodium methoxide under a temperature condition of 60-100 DEG C; then synthesizing 1,5-diazacyclooctane bromate from 1,5-bis(p-toluenesulfonyl)-1,5-diazacyclooctane, phenol and hydroacetic acid; and finally, synthesizing 1,5-diazacyclooctane from 1,5-diazacyclooctane bromate and sodium methoxide. According to the method, the yield of the 1,5-bis(p-toluenesulfonyl)-1,5-diazacyclooctane can be increased, and the reaction time for synthesizing the 1,5-diazacyclooctane can be shortened.

Synthesis, characterization, and copper(II) chelates of 1,11-dithia-4,8-diazacyclotetradecane

Synthesis of 1,11-dithia-4,8-diazacyclotetradecane (L1), a constitutional isomer of the macrocyclic [14]aneN2S2 series, is accompanied with reaction and method optimization. Chelation of L1 with copper(II) provided assessment of latt

Gold-Catalyzed Regiodivergent [2 + 2 + 2]-Cycloadditions of Allenes with Triazines

Gold-catalyzed regiodivergent cycloadditions of functionalized allenes with 1,3,5-triazines, providing diverse N-heterocycles in moderate to excellent yields under mild reaction conditions, are reported. Importantly, different types of allenes exhibit distinct selectivity and reactivity for the reactions. Mechanistic investigations reveal that all of the cycloadditions proceed through a stepwise [2 + 2 + 2]-cycloaddition process.

Tuning Side Arm Electronics in Unsymmetrical Cyclotriazadisulfonamide (CADA) Endoplasmic Reticulum (ER) Translocation Inhibitors to Improve their Human Cluster of Differentiation 4 (CD4) Receptor Down-Modulating Potencies

Cyclotriazadisulfonamide prevents HIV entry into cells by down-modulating surface CD4 receptor expression through binding to the CD4 signal peptide. According to a two-site binding model, 28 new unsymmetrical analogues bearing a benzyl tail group and nine

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).

Synthesis and characterisation of a mesocyclic tripodal triamine ligand

Meso- and macrocyclic polydentate amine ligands have been widely explored in oxidation catalysis and for the stabilization of unstable metal-superoxide, -peroxide, and -oxo intermediates. Herein we report on the design and synthesis of a novel mesocyclic,

Quantitative structure-activity relationships studies for prediction of antimicrobial activity of synthesized disulfonamide derivatives

A new series of disulfonamides were synthesized and assayed as antimicrobial agents against Staphylococcus aureus, Bacillus cereus, and Escherichia coli. The quantitative structure-activity relationship analysis (QSAR) was applied to find out the correlat

Unsymmetrical cyclotriazadisulfonamide (CADA) compounds as human CD4 receptor down-modulating agents

Cyclotriazadisulfonamide (CADA) inhibits HIV at submicromolar levels by specifically down-modulating cell-surface and intracellular CD4. The specific biomolecular target of CADA compounds is unknown, but previous studies led to an unsymmetrical binding model. To test this model, methods were developed for effective synthesis of diverse, unsymmetrical CADA compounds. A total of 13 new, unsymmetrical target compounds were synthesized, as well as one symmetrical analogue. The new compounds display a wide range of potency for CD4 down-modulation in CHO-CD4-YFP cells. VGD020 (IC50 = 46 nM) is the most potent CADA compound discovered to date, and VGD029 (IC50 = 730 nM) is the most potent fluorescent analogue. Structure-activity relationships are analyzed from the standpoint of additive or nonadditive energy effects of different substituents. They appear to be consistent with the zipper-type mechanism in which entropy costs are reduced for additional stabilizing interactions between the small molecule and its protein target.

A highly efficient synthesis of sulphonamide derivatives in the presence of n-methyl-2-pyrrolidone

The sulphonamide derivatives are synthesized by two component condensation of alkyl bromide and sodium arylsulphonamide using N-methyl-2-pyrrolidone (NMP) as a reaction medium. This method results in high yields without the formation of unwanted side products, and expanding substrate scopes. Copyright

Copper-catalyzed 1,2-double amination of 1-halo-1-alkynes. Concise synthesis of protected tetrahydropyrazines and related heterocyclic compounds

Reaction of N,N′-di(p-toluenesulfonyl)-1,2-diamine, 1-bromo-1-alkyne, K3PO4, and a catalytic amount of CuI in hot DMF afforded N,N′-di(p-toluenesulfonyl)-1,2,3,4-tetrahydropyrazines in good yields. The reaction most likely involves (i) monoalkynylation of the diamine derivative with 1-bromo-1-alkyne, and (ii) 6-endo-dig ring closure between the acetylenic bond and another sulfonylamine moiety of the diamine. When the starting 1,2-diamine derivative was replaced with N,N′-di(p-toluenesulfonyl)-1,3-diamine or N-(p-toluenesulfonyl)-2-amino-1-ethanol, the corresponding seven-membered diazacycle or six-membered N,O-heterocycle was produced. In addition, 1,1-dibromo-1-alkene could be used in place of 1-bromo-1-alkyne. Copyright