1939-76-0

Upstream product

• 942199-56-6 2-chloro-5-cyanobenzene-1-sulfonyl chloride 
• 53312-79-1 3-amino-4-chloro-benzonitrile 
• 939-80-0 4-chloro-3-nitrobenzonitrile 
• 623-03-0 4-Cyanochlorobenzene 
• 70049-77-3 3-(aminosulfonyl)-4-chlorobenzoyl chloride 
• 2455-92-7 4-chloro-3-sulfamoylbenzamide 
• 1205-30-7 4-chloro-3-sulphamoylbenzoic acid 

Downstream Products

• 59210-41-2 5-cyano-2-(4-methyl-piperazin-1-yl)-benzenesulfonamide 
• 3279-81-0 2-chloro-5-formyl-benzenesulphonamide 
• 70049-79-5 4-chloro-3-sulfamoylphenyl-2-methyl-3-indolyl-ketonimine hydrochloride 
• 1254304-28-3 C₁₆H₇Cl₂F₃N₄O₃S 

Relevant academic research and scientific papers

Research on controllable degradation of sulfonylurea herbicides

In order to seek ecologically safer and environmentally benign sulfonylurea herbicides (SU), insight into the structure/bioassay/soil degradation tri-factor relationship was first established. With the introduction of various groups (alkyl, nitro, halogen, cyano etc.) at the 5th position of its benzene ring, structural derivatives of chlorsulfuron were designed, synthesized, and evaluated for their herbicidal activity. The structures of the title compounds were confirmed by infrared spectroscopy, ultraviolet spectroscopy, 1H and 13C NMR, mass spectrometry, elemental analysis and X-ray diffraction. Bioassay results confirmed that most derivatives retained their superior herbicidal activities in comparison with chlorsulfuron. After investigating the soil degradation behavior of each molecule under set conditions, it was found that structures with electron-withdrawing substituents at the 5th position of the benzene ring retained their long degradation half-lives, yet the introduction of electron-donating substituents accelerated the degradation rate. These results will provide a valuable clue to further explore the potential controllable degradation of SU and other herbicides, and to discover novel herbicides that are favorable for environmentally and ecologically sustainable development.

1,4,2-Benzo/pyridodithiazine 1,1-dioxides structurally related to the ATP-sensitive potassium channel openers 1,2,4-Benzo/pyridothiadiazine 1,1-dioxides exert a myorelaxant activity linked to a distinct mechanism of action

The synthesis of diversely substituted 3-alkyl/aralkyl/arylamino-1,4,2- benzodithiazine 1,1-dioxides and 3-alkylaminopyrido[4,3-e]-1,4,2-dithiazine 1,1-dioxides is described. Their biological activities on pancreatic β-cells and on smooth muscle cells were compared to those of the reference ATP-sensitive potassium channel (KATP channel) openers diazoxide and 7-chloro-3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxide. The aim was to assess the impact on biological activities of the replacement of the 1,2,4-thiadiazine ring by an isosteric 1,4,2-dithiazine ring. Most of the dithiazine analogues were found to be inactive on the pancreatic tissue, although some compounds bearing a 1-phenylethylamino side chain at the 3-position exerted a marked myorelaxant activity. Such an effect did not appear to be related to the opening of KATP channels but rather reflected a mechanism of action similar to that of calcium channel blockers. Tightly related 3-(1-phenylethyl)sulfanyl-4H-1,2,4-benzothiadiazine 1,1-dioxides were also found to exert a pronounced myorelaxant activity, resulting from both a K ATP channel activation and a calcium channel blocker mechanism. The present work highlights the critical importance of an intracyclic NH group at the 4-position, as well as an exocyclic NH group linked to the 3-position of the benzo- and pyridothiadiazine dioxides, for activity on KATP channels.

Benzene-sulphonamide derivatives and their uses

Benzene-sulphonamide derivatives complying with the general formula (I): in which the different symbols have different meanings, their optical isomers and the salts pharmacologically acceptable of these derivatives, as well as their uses for drug manufacture and as radiolabelled pharmacological tools of the thromboxan A2 receptors.