4911-65-3Relevant academic research and scientific papers
Increasing Complexity: A Practical Synthetic Approach to Three-Dimensional, Cyclic Sulfoximines and First Insights into Their in Vitro Properties
Boulard, Emilie,Ganzer, Ursula,Lücking, Ulrich,Lienau, Philip,Oertel, Luisa,Sch?fer, Martina,Zibulski, Vivien
, (2020/03/23)
A short synthetic approach with broad scope to access five- to seven-membered cyclic sulfoximines in only two to three steps from readily available thiophenols is reported. Thus, simple building blocks were converted to complex molecular structures by a s
Synthesis of α-Cyano and α-Sulfonyl Cyclic Ethers via Intramolecular Reactions of Peroxides with Sulfone- And Nitrile-Stabilized Carbanions
Horn, Alissa,Dussault, Patrick H.
, p. 14611 - 14626 (2019/11/13)
The intramolecular reaction of carbon nucleophiles with oxygen-centered electrophiles has been little explored outside of nucleophilic epoxidation. We now report the synthesis of sulfonyl- and cyano-substituted oxacycles via intramolecular reaction of sul
Pummerer Synthesis of Chromanes Reveals a Competition between Cyclization and Reductive Chlorination
Acosta-Guzmán, Paola,Rodríguez-López, Alvaro,Gamba-Sánchez, Diego
supporting information, p. 6903 - 6908 (2019/09/30)
The competition between an unprecedented reductive chlorination and the Pummerer reaction was studied and applied to the synthesis of benzofused oxygen heterocycles including 3-aminochromanes and in the intramolecular chlorination of activated aromatic ri
NR2B SELECTIVE NMDA-RECEPTOR ANTAGONISTS FOR TREATMENT OF IMMUNE-MEDIATED INFLAMMATORY DISEASES
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Paragraph 160, (2017/03/21)
The present invention provides novel means and methods for treatment auf immunemediated inflammatory diseases.
Scandium(III) Triflate-Catalyzed anti-Markovnikov Hydrothiolation of Functionalized Olefins
Kuciski, Krzysztof,Pawluc, Piotr,Hreczycho, Grzegorz
, p. 3936 - 3942 (2016/01/25)
Scandium(III) triflate promoted highly selective addition of thiols to functionalized olefins under mild conditions. The addition follows anti-Markovnikov regioselectivities, which are unusual for Lewis acids-catalyzed hydrothiolation. This reaction marks broad functional groups tolerance, which opens a beneficial synthetic route to functionalized and biologically active thio-compounds. This method is broadly applicable and offers a simple work-up in the green manner.
Gas-phase S-alkylation of benzenethiol with aliphatic alcohols, ethers, esters, alkyl halides and olefins over halide cluster catalysts of Groups 5 and 6 transition metals
Nagashima, Sayoko,Kudo, Kentaro,Yamazaki, Hitomi,Kamiguchi, Satoshi,Chihara, Teiji
, p. 50 - 56 (2013/02/25)
Benzenethiol was reacted with methanol under a hydrogen stream over [(Nb6Cl12)Cl2(H2O) 4]·6H2O supported on silica gel. Catalytic activity of the cluster commenced above 250 °C, yielding methyl phenyl sulfide. The selectivity was 98% at 400 °C. Molybdenum, tantalum and tungsten halide clusters with the same octahedral metal framework also catalyzed the reaction. Primary alcohols with shorter alkyl chains were effective reagents for the S-alkylation. Aliphatic ethers, dialkyl carbonates, orthoesters and alkyl halides were effective reagents for the S-alkylation. When 1-hexene was applied to the reaction, spontaneous and catalytic S-alkylation proceeded simultaneously above 200 °C, yielding n-hexyl phenyl sulfide. When alkyl acetates were subjected to this reaction, the niobium cluster afforded S-phenyl thioacetate, and the other clusters afforded alkyl phenyl sulfides selectively. A Br?nsted acid site attributable to a hydroxo ligand, which is formed on the cluster complex by thermal activation, is proposed as the active site of the catalysts.
Diastereoselective synthesis of tetrahydrofurans from Aryl 3-chloropropylsulfoxides and aldehydes
Komsta, Zofia,Barbasiewicz, Michal,Makosza, Mieczyslaw
supporting information; experimental part, p. 3251 - 3259 (2010/08/19)
Carbanions of aryl 3-chloropropylsulfoxides react with nonenolizable aldehydes to give 2,3-disubstituted tetrahydrofurans. Deprotonation of the sulfoxides carried out in the presence of aldehydes results in the addition of the carbanions to the carbonyl group of the aldehydes, followed by 1,5-intramolecular substitution of the resulting aldol-type anion to produce the tetrahydrofuran ring. The 2-aryl and 3-arylsulfinyl substituents are always in trans relation, and the reaction proceeds with high diastereoselectivity also in respect to the chiral sulfur atom. The diastereoselectivity is attributed to the cyclic transition state of the aldol addition and increases when the aromatic ring of the sulfoxide contains electron-withdrawing substituents, whereas that of the aldehyde has electron-donating groups.
NR2B-SELECTIVE NMDA-RECEPTOR ANTAGONISTS
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Page/Page column 46, (2010/11/05)
The present invention relates to compounds according to general formula (I) and pharmaceutical compositions comprising compounds according to general formula (I).
Synthesis and QSAR studies on hypotensive 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines
Saxena, Anil K.,Rao, Jyoti,Chakrabarty, Ruchika,Saxena, Mridula,Srimal
, p. 1708 - 1712 (2007/10/03)
A series of 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines has been synthesized and evaluated for hypotensive activity. The QSAR studies indicate that resonance and hydrophobic parameters of the aryl substituents are important
Synthesis and pharmacological evaluation of benzamide derivatives as selective 5-HT4 receptor agonists
Sonda, Shuji,Kawahara, Toshio,Katayama, Kenichi,Sato, Noriko,Asano, Kiyoshi
, p. 3295 - 3308 (2007/10/03)
It is thought that selective 5-HT4 receptor agonists-such as 4-amino-5-chloro-2-methoxy-N-[1-(6-oxo-6-phenylhexyl)piperidin-4-ylmethyl] benzamide (2)-have the ability to enhance both upper and lower gastrointestinal motility without any significant adverse effects. Modification of 2 was performed. Variation of the piperidin-4-ylmethyl moiety of 2 led to a decrease in the binding affinity for the 5-HT4 receptor. Following conversion of the carbonyl group on the benzoyl part to a hydroxyl or sulfoxide group, the binding affinity for the 5-HT4 receptor was retained although the effect on defecation was reduced. Many of the 4-amino-5-chloro-2-methoxy-N- (piperidin-4-ylmethyl)benzamides that had a ether or sulfide moiety in the side-chain part at the 1-position of the piperidine exhibited high affinity for the 5-HT4 receptor. Among these, phenylthio 41c and benzylthio derivative 44 were selective 5-HT4 receptor agonists, and had a similar effect on defecation to compound 2.
