73300-75-1

Upstream product

• 371-69-7 ethyl fluorosulfonate 
• 114086-65-6 tetrabutylammonium diethylphosphorylmethanesulphonate 
• 1825-62-3 ethyl trimethylsilyl ether 
• 60812-40-0 (dichlorophosphoryl)methanesulfonyl chloride 
• 814-49-3 diethyl chlorophosphate 
• 62-50-0 Ethyl methanesulfonate 
• 683-08-9 Diethyl methylphosphonate 
• 73300-71-7 phosphonomethanesulfonic acid 
• 122-52-1 triethyl phosphite 

Downstream Products

• 114086-75-8 ethyl 2,2-pentamethylenevinylsulphonate 
• 114086-66-7 Ethyl 2-(p-chlorophenyl)vinylsulphonate 
• 73300-79-5 ethyl 2-(p-chlorophenyl)vinylsulphonate 
• 210428-01-6 (E)-(R)-3-tert-Butoxycarbonylamino-4-(tert-butyl-diphenyl-silanyloxy)-but-1-ene-1-sulfonic acid ethyl ester 
• 210428-15-2 (E)-(S)-3-tert-Butoxycarbonylamino-5-(trityl-carbamoyl)-pent-1-ene-1-sulfonic acid ethyl ester 
• 335281-12-4 2-(2-chlorophenyl)ethanesulfonic ethyl ester 
• 1094678-18-8 (E)-methyl 2-(6'-[ethoxysulfonyl]hexa-1'-5'-dien-2'-yl)benzoate 
• 1094678-16-6 (E)-methyl 2-(5'-[ethoxysulfonyl]pent-4'-enoyl)benzoate 
• 1239479-58-3 C₂₆H₄₃NO₆S 

Relevant academic research and scientific papers

Synthesis of tailored perfluoro unsaturated monomers for potential applications in proton exchange membrane preparation

The aim of the present work is the synthesis and characterization of new perfluorinated monomers bearing, similarly to Nafion, acidic groups for proton transport for potential and future applications in proton exchange membrane (PEM) fuel cells. To this e

Novel PTP1B enzyme inhibitor, preparation method and applications thereof

The present invention provides a novel PTP1B enzyme inhibitor, a preparation method and applications thereof, and particularly discloses a class of bis 2-substituted ethylene sulfonate compounds and a preparation method thereof, and uses of the bis 2-substituted ethylene sulfonate compounds as the PTP1B enzyme activity inhibitor. According to the present invention, the prepared novel compound has good PTP1B enzyme activity inhibition effect, and has the application value in preparation of drugs for treatment and prevention of diabetes and obesity.

Proteasome inhibition by new dual warhead containing peptido vinyl sulfonyl fluorides

The success of inhibition of the proteasome by formation of covalent bonds is a major victory over the long held-view that this would lead to binding the wrong targets and undoubtedly lead to toxicity. Great challenges are now found in uncovering ensembles of new moieties capable of forming long lasting ties. We have introduced peptido sulfonyl fluorides for this purpose. Tuning the reactivity of this electrophilic trap may be crucial for modulating the biological action. Here we describe incorporation of a vinyl moiety into a peptido sulfonyl fluoride backbone, which should lead to a combined attack of the proteasome active site threonine on the double bond and the sulfonyl fluoride. Although this led to strong proteasome inhibitors, in vitro studies did not unambiguously demonstrate the formation of the proposed seven-membered ring structure. Possibly, formation of a seven-membered covalent adduct with the proteosomal active site threonine can only be achieved within the context of the enzyme. Nevertheless, this dual warhead concept may provide exclusive possibilities for duration and selectivity of proteasome inhibition.

Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase

A series of α-ketooxazoles incorporating electrophiles at the C5 position of the pyridyl ring of 2 (OL-135) and related compounds were prepared and examined as inhibitors of fatty acid amide hydrolase (FAAH) that additionally target the cytosolic port Cys269. From this series, a subset of the candidate inhibitors exhibited time-dependent FAAH inhibition and noncompetitive irreversible inactivation of the enzyme, consistent with the targeted Cys269 covalent alkylation or addition, and maintained or enhanced the intrinsic selectivity for FAAH versus other serine hydrolases. A preliminary in vivo assessment demonstrates that these inhibitors raise endogenous brain levels of anandamide and other FAAH substrates upon intraperitoneal (i.p.) administration to mice, with peak levels achieved within 1.5-3 h, and that the elevations of the signaling lipids were maintained >6 h, indicating that the inhibitors effectively reach and remain active in the brain, inhibiting FAAH for a sustained period.

METHODS OF REDUCING VIRULENCE IN BACTERIA

A method of reducing virulence in a bacterium comprising at least one of a GacS/GacA-type system, a HrpX/HrpY-type system, a T3SS-type system, and a Rsm-type system, the method comprising contacting the bacterium with an effective amount of a compound described herein.

INHIBITORS OF E1 ACTIVATING ENZYMES

This invention relates to compounds that inhibit El activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand

The discovery and SAR of ketopiperazino methylazaindole factor Xa inhibitors are described. Structure-activity data suggesting that this class of inhibitors does not bind in the canonical mode were confirmed by an X-ray crystal structure showing the neutral haloaromatic bound in the S1 subsite. The most potent azaindole, 33 (RPR209685), is selective against related serine proteases and attains higher levels of exposure upon oral dosing than comparable benzamidines and benzamidine isosteres. Compound 33 was efficacious in the canine AV model of thrombosis.

Methods of using α-phosphonosulfonate squalene synthetase inhibitors including the treatment of atherosclerosis and hypercholesterolemia

α-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula STR1 wherein R2 is OR5 or R5a ; R3 and R5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R5a is H, alkyl, arylalkyl or aryl; R4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.

A NEW SYNTHESIS OF α,β-UNSATURATED SULPHONATES AND THEIR STEREOSELECTIVE CONVERSION INTO TRANS-α,β-EPOXYSULPHONATES.

Diethylphosphoryl methanesulphonates 2 and 4 were readily converted into α,β-unsaturated sulphonates by succesive treatment with n-BuLi and aldehydes or ketones.Epoxidation of esters 5 with t-butyl hydroperoxide in the presence of Triton B yielded stereoselectively salts of trans-α,β-epoxysulphonic acids.

SYNTHESIS OF α,β-UNSATURATED SULPHONATES VIA THE WITTIG-HORNER REACTION

A general and practical method of synthesis of α,β-unsaturated sulphonates (25 examples) by the Wittig-Horner reaction is described.Reactions with the salts 2 and carbonyl compounds are not very stereoselective.On the contrary, reactions with esters 1 gave high yields of (E)-α,β-unsaturated sulphonic esters.