87708-16-5

Usage

InChI:InChI=1/C9H10N2O4S/c12-9-11(6-7-15-9)16(13,14)10-8-4-2-1-3-5-8/h1-5,10H,6-7H2

Upstream product

• 87708-04-1 N-(chloro-2 ethoxycarbonyl) N'-(phenyl) sulfamide 
• 1189-71-5 isocyanate de chlorosulfonyle 
• 62-53-3 aniline 
• 107-07-3 2-chloro-ethanol 
• 540-51-2 2-bromoethanol 

Downstream Products

• 1245920-58-4 C₁₇H₂₀N₂O₂S 
• 587-14-4 N,N'-diphenylsulfamide 
• 69705-83-5 N-isopropyl-N'-phenyl-sulfamide 

Relevant academic research and scientific papers

Histone deacetylase inhibitors and its preparation method and use thereof

The invention discloses a histone deacetylase inhibitor and its preparation method and use, the invention discloses a compound of the formula I as shown, or its crystalline form, or its pharmaceutically acceptable salt, or solvate thereof, or prodrug thereof, or its metabolic product. The invention of the formula I illustrated new compound, has shown good deacetylase inhibition activity, with the histone deacetylase for clinical treatment of diseases associated with abnormal activity of a new pharmaceutical may be.

Histone deacetylase inhibitors and its preparation method and use thereof

The invention discloses a histone deacetylase inhibitor and its preparation method and use, the invention discloses a compound of the formula I as shown, or its crystalline form, or its pharmaceutically acceptable salt, or solvate thereof, or prodrug thereof, or its metabolic product. The invention of the formula I illustrated new compound, has shown good deacetylase inhibition activity, with the histone deacetylase for clinical treatment of diseases associated with abnormal activity of a new pharmaceutical may be.

FUSED-RING COMPOUNDS, PHARMACEUTICAL COMPOSITION AND USES THEREOF

This disclosure is related to a fused-ring compound of formula (I) and/or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the fused ring compound of formula (I) and/or a pharmaceutically acceptable salt thereof, preparation methods thereof, and use thereof in modulating activity of indoleamine 2, 3-dioxygenase (IDO) and/or tryptophan 2, 3-dioxygenase (TDO). This disclosure further provides methods of treating IDO and/or TDO-associated diseases, including cancer, viral infection and autoimmune diseases.

Discovery of 3-benzyl-1,3-benzoxazine-2,4-dione analogues as allosteric mitogen-activated kinase kinase (MEK) inhibitors and anti-enterovirus 71 (EV71) agents

Enterovirus 71 (EV71) is a kind of RNA virus and one of the two causes of Hand, foot and mouth disease (HFMD). Inhibitors that target key components of Ras/Raf/MEK/ERK pathway in host cells could impair replication of EV71. A series of 3-benzyl-1,3-benzoxazine-2,4-diones were designed from a specific MEK inhibitor G8935, by replacing the double bond between C3 and C4 within the coumarin scaffold with amide bond. One compound (9f) showed submicromolar inhibitory activity among the 12 derivatives. Further optimization on 9f led to two active compounds (9k and 9m) with nanomolar bioactivities (55?nM and 60?nM). The results of enzymatic assays also demonstrated that this series of compounds were allosteric inhibitors of unphosphorylated MEK1. The binding mode of compound 9k was predicted by molecular dynamic simulation and the key interactions were same as published MEK1/2 allosteric inhibitors. In the cell-based assays, compounds 9k and 9m could effectively suppress the ERK1/2 pathway, expression of EV71 VP1, and EV71 induced cytopathic effect (CPE) in rhabdomyosarcoma (RD) cells.

Copper-catalyzed oxidative amination and allylic amination of alkenes

Enamines and enamides are useful synthetic intermediates and common components of bioactive compounds. A new protocol for their direct synthesis by a net alkene C-H amination and allylic amination by using catalytic Cu II in the presence of MnO2 is reported. Reactions between N-aryl sulfonamides and vinyl arenes furnish enamides, allylic amines, indoles, benzothiazine dioxides, and dibenzazepines directly and efficiently. Control experiments further showed that MnO2 alone can promote the reaction in the absence of a copper salt, albeit with lower efficiency. Mechanistic probes support the involvement of nitrogen-radical intermediates. This method is ideal for the synthesis of enamides from 1,1-disubstituted vinyl arenes, which are uncommon substrates in existing oxidative amination protocols. A new protocol for the direct synthesis of enamides and allylic amines by oxidative N-H/C-H coupling of N-sulfonylanilines with vinylarenes is presented. The reaction works in both inter- and intramolecular modes and is catalyzed by copper salts by using MnO2 as the stoichiometric oxidant (see scheme). Nitrogen heterocycles including indoles, benzothiazine dioxides, and dibenzazepines can be formed. Copyright

Synthesis, crystal structure and antibacterial evaluation of substituted perhydro-1, 3-oxazin-2-ones containing N-phenylsulfonamide

The synthesis of a new series of TV-substituted perhydro-1,3-oxazin-2-ones containing V-phenylsulfonamide is described. The compounds 7a-7f were obtained in a one-pot reaction from chlorosulfonyl isocyanate, selected 1, 3-halogenoalcohols and various aromatic amines in alkaline conditions, to give the target N-heterocyclic 6-membered ring compounds with good yields. The X-ray crystal structure of N-[(N-4-fluorophenyl)sulfamoyl]perhydro-1, 3-oxazin-2-one 7d was solved. All the synthesized compounds have been screened for their invitro antibacterial activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Structures of 7d and 6e can be further optimized to give new potent antibacterial agents with structures significantly different from those of existing classes of antibiotics. The Japan Institute of Heterocyclic Chemistry.

Modular synthesis of 1,2-Diamine derivatives by palladium-Catalyzed aerobic oxidative cyclization of allylic sulfamides

Chemical equation presented Allylic sulfamides undergo aerobic oxidative cyclization at room temperature, mediated by a Pd(O 2CCF3)2/DMSO catalyst system in tetrahydrofuran. The cyclic sulfamide products are readily converted into 1,2-diamines, and substrates derived from chiral allylic amines cyclize with very high diastereoselectivity.

SULFAMIDES AS ZAP-70 INHIBITORS

The invention relates to compounds offormula(I),wherein X,R1,R2,R3,R8,R9 have the meaning as cited in the description and the claims.Said compounds are useful as inhibitors of ZAP-70 for the treatment orprophylaxis of immunological, inflammatory, autoimmu

Mild and safer preparative method for nonsymmetrical sulfamides via N-sulfamoyloxazolidinone derivatives: Electronic effects affect the transsulfamoylation reactivity

Sulfamides (R1R2N-SO2-NR3R 4) are traditionally prepared by using strong electrophilic and hazardous reagents such as N-sulfamoyl chloride, sulfonyl chloride, phosphorus oxychloride, or phosphorus pentachloride. We report here a safer and more convenient synthetic methodology for large-scale preparation of sulfamides using the N-substituted oxazolidin-2-one derivatives 5 as synthetic equivalent of the corrosive and hazardous N-sulfamoyl chloride. The scope of the use of N-sulfamoyloxazolidinones to prepare nonsymmetrical sulfamides is explored.

Derives de l'isocyanate de chlorosulfonyle. Synthese, structure et activite biologique d'halogeno-2 ethoxycarbonylsulfamides

New 2-chloroethoxycarbonylsulfamides are synthesized in a two step reaction from C.S.I., haloethanol and various primary and secondary amines.Cyclization of these sulfamides in basic medium gives the corresponding sulfamyl-oxazolidinones.All structures are established by IR, NMR, MS and RX diffraction data.The antitumor activity of the products towards LI210 is reported.