6461-78-5

Upstream product

• 127-63-9 diphenyl sulphone 
• 63113-57-5 3-sulfodiphenyl sulfone 
• 98-09-9 benzenesulfonyl chloride 
• 71-43-2 benzene 

Downstream Products

• 915755-18-9 C₂₁H₁₉NO₄S₂ 
• 93041-54-4 3-(phenylsulfonyl)benzenesulfonamide 
• 1260488-20-7 N-methyl-3-(phenylsulfonyl)benzenesulfonamide 

Relevant academic research and scientific papers

Inhibitors of the salicylate synthase (Mbti) from Mycobacterium tuberculosis discovered by high-throughput screening

A simple steady-state kinetic high-throughput assay was developed for the salicylate synthase MbtI from Mycobacterium tuberculosis, which catalyzes the first committed step of mycobactin biosynthesis. The mycobactins are small-molecule iron chelators produced by M. tuberculosis, and their biosynthesis has been identified as a promising target for the development of new antitubercular agents. The assay was miniaturized to a 384-well plate format and high-throughput screening was performed at the National Screening Laboratory for the Regional Centers of Excellence in Biodefense and Emerging Infectious Diseases (NSRB). Three classes of compounds were identified comprising the benzisothiazolones (class I), diarylsulfones (class II), and benzimidazole-2-thiones (class III). Each of these compound series was further pursued to investigate their biochemical mechanism and structure-activity relationships. Benzimidazole-2-thione 4 emerged as the most promising inhibitor owing to its potent reversible inhibition.

Identification of diarylsulfone sulfonamides as secreted frizzled related protein-1 (sFRP-1) inhibitors

Inhibitor of secreted frizzled related protein-1 (sFRP-1) would be a novel potential osteogenic agent, since loss of sFRP-1 affects osteoblast proliferation, differentiation, and activity, resulting in improved bone mineral density, quality, and strength. We have identified small molecule diarylsulfone sulfonamide derivatives as sFRP-1 inhibitors. Structure-activity relationship generated for various regions of the scaffold was utilized to improve the biochemical profile, resulting in the identification of potent selective analogues, such as 16 with desirable pharmaceutical profile.

Synthesis of new sulfonyl chlorides on the basis of substituted diphenyl sulfones

-Sulfonation of substituted diphenyl sulfones with excess chlorosulfonic acid at 100°C yields as a rule the corresponding bis-sulfonyl chlorides. The reaction with an equimolar amount of 20% oleum yields products of sulfonation of only one benzene ring.

Guanidine derivatives compositions and use

Compounds of the formula STR1 wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.

CHLOROSULFONATION OF SOME DIPHENYL DERIVATIVES

Benzophenone (1), diphenyl sulfone, and 4-nitro-2'-chloro- and 4-nitro-2',6'-dichlorophenyl ethers (23,24) have been chlorosulfonated.The direct yield of benzophenone-3,3'-disulfonyl chloride (2) was low, the majority of product was the disulfonic acid.Diphenyl sulfone (11) with a large amount of chlorosulfonic acid (8 mols) at 140 deg gave the 3,3'-disulfonyl chloride (12).With less reagent (6 mols) at 90 deg a mixture of the 3-sulfonyl chloride (21) and diphenyl sulfone was formed.Subsequent reaction with sodium azide gave the 3-sulfonyl azide (22).The diphenyl ether sulfonyl chlorides (25,26) were very susceptible to hydrolysis, especially (26) which probably accounts for the low yield obtained (31percent).The various sulfonyl chlorides were characterized as amides, azides, hydrazides and hydrazones (Tables I-III) and their i.r., n.m.r., and mass spectral data are included.