53606-38-5

Upstream product

• 68-12-2 N,N-dimethyl-formamide 
• 1569-69-3 Cyclohexanethiol 
• 15164-44-0 p-(iodophenyl)carboxaldehyde 
• 459-57-4 4-fluorobenzaldehyde 

Downstream Products

• 1174009-35-8 4-(cyclohexylsulfonyl)benzaldehyde 
• 1174009-33-6 cyclohexyl(4-(dimethoxymethyl)phenyl)sulfane 
• 97830-78-9 2-<4-(2-Diaethylamino-aethoxy)-phenyl>-3-<4-cyclohexylmercaptophenyl>-acrylnitril 

Relevant academic research and scientific papers

Nature of the copper-oxide-mediated C-S cross-coupling reaction: Leaching of catalytically active species from the metal oxide surface

Copper-oxide-catalyzed cross-coupling reaction is a well-known strategy in heterogeneous catalysis. A large number of applications have been developed, and catalytic cycles have been proposed based on the involvement of the copper oxide surface. In the present work, we have demonstrated that copper(I) and copper(II) oxides served as precursors in the coupling reaction between thiols and aryl halides, while catalytically active species were formed upon unusual leaching from the oxide surface. A powerful cryo-SEM technique has been utilized to characterize the solution-state catalytic system by electron microscopy. A series of different experimental methods were used to reveal the key role of copper thiolate intermediates in the studied catalytic reaction. The present study shows an example of leaching from a metal oxide surface, where the leaching process involved the formation of a metal thiolate and the release of water. A new synthetic approach was developed, and many functionalized sulfides were synthesized with yields of up to 96%, using the copper thiolate catalyst. The study suggests that metal oxides may not act as an innocent material under reaction conditions; rather, they may represent a source of reactive species for solution-state homogeneous catalysis.

Structure-Based Optimization of N-Substituted Oseltamivir Derivatives as Potent Anti-Influenza A Virus Agents with Significantly Improved Potency against Oseltamivir-Resistant N1-H274Y Variant

Due to the emergence of highly pathogenic and oseltamivir-resistant influenza viruses, there is an urgent need to develop new anti-influenza agents. Herein, five subseries of oseltamivir derivatives were designed and synthesized to improve their activity toward drug-resistant viral strains by further exploiting the 150-cavity in the neuraminidases (NAs). The bioassay results showed that compound 21h exhibited antiviral activities similar to or better than those of oseltamivir carboxylate (OSC) against H5N1, H5N2, H5N6, and H5N8. Besides, 21h was 5- to 86-fold more potent than OSC toward N1, N8, and N1-H274Y mutant NAs in the inhibitory assays. Computational studies provided a plausible rationale for the high potency of 21h against group-1 and N1-H274Y NAs. In addition, 21h demonstrated acceptable oral bioavailability, low acute toxicity, potent antiviral activity in vivo, and high metabolic stability. Overall, the above excellent profiles make 21h a promising drug candidate for the treatment of influenza virus infection.

Compounds Having CRTH2 Antagonist Activity

Compounds of general formula (I) wherein W is chloro or fluoro; Z is a group SO2R1; wherein R1 is —C3-C8 cycloalkyl or heterocyclyl optionally substituted with one or more substituents chosen from hal

COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY

Compounds of general formula (I): wherein W is chloro or fluoro; Z is a group SO2R1; wherein R1 is -C3-C8 cycloalkyl or heterocyclyl optionally substituted with one or more substituents chosen from halo, -CN, -C1-C6 alkyl, -SOR3, -SO2R3, -SO2N(R2)2, -N(R2)2, -NR2C(O)R3, -CO2R2, -CONR2R3, -NO2, -OR2, -SR2, -O(CH2)POR2, and - O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, -Ci-C6 alkyl, -C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, -C1-C6 alkyl, -C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.