41067-80-5

Upstream product

• 110-91-8 morpholine 
• 452905-58-7 ethenesulfonic acid pentafluorophenyl ester 
• 1622-32-8 2-Chloroethanesulfonyl chloride 

Downstream Products

• 958297-92-2 7H-indolo[2,1-a][2]benzazepine-10-carboxylic acid, 13-cyclohexyl-3-methoxy-6-(4-morpholinylsulfonyl)-, methyl ester 
• 173336-66-8 2-(morpholinosulfonyl)ethanamine 
• 1257106-59-4 (3R)-3-{4-[2-(morpholine-4-sulfonyl)-vinyl]-phenyl}-cyclopentanone 
• 87975-63-1 Ethyl-[2-(morpholine-4-sulfonyl)-3-phenyl-oxiranylmethyl]-amine 
• 87975-43-7 4-(1-Benzyl-aziridine-2-sulfonyl)-morpholine 
• 87975-18-6 Benzyl-[2-bromo-2-(morpholine-4-sulfonyl)-ethyl]-amine 
• 87975-17-5 [2-Bromo-2-(morpholine-4-sulfonyl)-ethyl]-cyclohexyl-amine 
• 87975-42-6 4-(1-Cyclohexyl-aziridine-2-sulfonyl)-morpholine 

Relevant academic research and scientific papers

Reactions of Aminoacetals with C-Nucleophiles as a New Method for the Synthesis of Di(het)arylmethane Derivatives with a Taurine Fragment

Abstract: Based on the acid-catalyzed reaction of functionalized aminoacetals with C-nucleophiles, a series of new diarylmethane derivatives with a taurine fragment were synthesized, the structure of which was established by NMR spectroscopy method.

Preparation of Functionalized α,β-Unsaturated Sulfonamides via Olefin Cross-Metathesis

The synthesis of functionalized α,β-unsaturated sulfonamides by means of cross-metathesis of vinyl sulfonamides and olefins has been developed. The reaction proceeds smoothly in the presence of Hoveyda-Grubbs catalyst and its nitro analogue, providing a w

Development of Selective Steroid Inhibitors for the Glucose-6-phosphate Dehydrogenase from Trypanosoma cruzi

Chagas disease is a parasitic infection affecting millions of people across Latin America, imposing a dramatic socioeconomic burden. Despite the availability of drugs, nifurtimox and benznidazole, lack of efficacy and incidence of side-effects prompt the identification of novel, efficient, and affordable drug candidates. To address this issue, one strategy could be probing the susceptibility of Trypanosoma parasites toward NADP-dependent enzyme inhibitors. Recently, steroids of the androstane group have been described as highly potent but nonselective inhibitors of parasitic glucose-6-phosphate dehydrogenase (G6PDH). In order to promote selectivity, we have synthesized and evaluated 26 steroid derivatives of epiandrosterone in enzymatic assays, whereby 17 compounds were shown to display moderate to high selectivity for T. cruzi over the human G6PDH. In addition, three compounds were effective in killing intracellular T. cruzi forms infecting rat cardiomyocytes. Altogether, this study provides new SAR data around G6PDH and further supports this target for treating Chagas disease.

Selective lysine modification of native peptides: Via aza-Michael addition

A series of vinylsulfonamides were synthesized and screened for site-selective modification of the ?-amino group of lysine-bearing free α-amine residues. N-Methyl-N-phenylethenesulfonamide has emerged as an applicable reagent and has been developed for efficient and highly selective modification of the lysine residue of native peptides in the presence of a free N-terminus via aza-Michael addition. We demonstrated that functional N-phenylvinylsulfonamide derivatives with a fluorescent moiety or drug could also be conjugated to the lysine residue of octreotide and insulin with high specificity, without modifying the N-terminus. Our method provides a promising strategy for site-selective lysine functionalization in native peptides with a free N-terminus.

Chemo- and Regioselective Direct Functional Group Installation through Catalytic Hydroxy Group Selective Conjugate Addition of Amino Alcohols to α,β-Unsaturated Sulfonyl Compounds

A chemoselective functional group installation through catalytic hydroxy group selective conjugate addition of amino alcohols to a variety of functionalized α,β-unsaturated sulfonyl derivatives was developed. Azide group installation for click chemistry and facile fluorescent labeling onto the less reactive hydroxy group demonstrated the synthetic utility of the present chemoselective catalysis. Moreover, chemo- and regioselective reaction of an unprotected amino diol was achieved for the first time.

AROMATIC HETEROCYCLIC DERIVATIVE HAVING TRPV4-INHIBITING ACTIVITY

A compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof is provided. The present invention is related to a compound represented by the formula (I). wherein R1a is substituted or unsubstituted alkyl or the like;

Cyclopropyl Fused Indolobenzazepine HCV NS5B Inhibitors

The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.

Synthese automatisee de l'ethenesulfonamide et du morpholinosulfonylethene

In a recent publication, Krutal and his col. have reported difficulties in preparing ethenesulfonamide, CH2=CHSO2NH2 (1).To overcome these difficulties we have developed a convenient and automatic synthesis of this simple reagent widely used for sulfoethylation.The same process has been used for the synthesis of a derivative, CH2=CHSO2NC4H8O.