340771-31-5Relevant academic research and scientific papers
Pyridylidene Amide Ru Complex for Selective Oxidation in Organic Synthesis
Bertini, Simone,Henryon, Dorothée,Edmunds, Andrew J. F.,Albrecht, Martin
supporting information, p. 1378 - 1382 (2022/02/23)
The ruthenium(II) bis(PYA) complex 1 (PYA = p-pyridylidene amide) is a powerful catalyst for the oxidation of sulfides to sulfones, of alkenes to carbonyl compounds, and of terminal alkynes to carboxylic acids by using NaIO4 as the terminal oxidant. The catalytic system shows a broad functional group tolerance and rate differences between alkyne and sulfide oxidation that are sufficiently large to effectively achieve selective sulfide oxidation with exquisite selectivity.
Selective Late-Stage Oxygenation of Sulfides with Ground-State Oxygen by Uranyl Photocatalysis
Li, Yiming,Rizvi, S. Aal-e-Ali,Hu, Deqing,Sun, Danwen,Gao, Anhui,Zhou, Yubo,Li, Jia,Jiang, Xuefeng
supporting information, p. 13499 - 13506 (2019/08/21)
Oxygenation is a fundamental transformation in synthesis. Herein, we describe the selective late-stage oxygenation of sulfur-containing complex molecules with ground-state oxygen under ambient conditions. The high oxidation potential of the active uranyl cation (UO22+) enabled the efficient synthesis of sulfones. The ligand-to-metal charge transfer process (LMCT) from O 2p to U 5f within the O=U=O group, which generates a UV center and an oxygen radical, is assumed to be affected by the solvent and additives, and can be tuned to promote selective sulfoxidation. This tunable strategy enabled the batch synthesis of 32 pharmaceuticals and analogues by late-stage oxygenation in an atom- and step-efficient manner.
Novel valdecoxib derivatives by ruthenium?II)-promoted 1, 3-dipolar cycloaddition of nitrile oxides with alkynes - Synthesis and COX-2 inhibition activity
Roscales, Silvia,Bechmann, Nicole,Holger Weiss, Daniel,K?ckerling, Martin,Pietzsch, Jens,Kniess, Torsten
supporting information, p. 534 - 544 (2018/03/28)
Novel valdecoxib-based cyclooxygenase-2 inhibitors were synthesized in one step via 1, 3-dipolar cycloaddition of nitrile oxides with a series of eleven aryl alkynes, six of them described for the first time. Application of Ru?II)-catalysis leads preferab
One-pot synthesis of 1, 2-disubstituted 4-, 5-, 6-, and 7-azaindoles from amino-o-halopyridines via n-arylation/sonogashira/cyclization reaction
Purifica??o, Sara I.,Pires, Marina J.D.,Rippel, Rafael,Santos, A. Sofia,Marques, M. Manuel B.
supporting information, p. 5118 - 5121 (2017/11/07)
A direct synthesis of several 1, 2-disubstituted 4-, 5-, 6-, and 7-azaindoles from available amino-o-halopyridines is described. This procedure involves a palladium-catalyzed N-arylation followed by a Sonogashira reaction and subsequent cyclization in a one-pot manner, exhibiting a wide scope and compatibility with electron-withdrawing and electron-donating groups. The strategy represents an advancement in azaindole chemistry with a straightforward approach toward 1, 2-disubstituted azaindoles, while avoiding complex N-arylations of hindered 2-substituted azaindoles and difficult purification steps of intermediates.
Transition-metal-free regioselective synthesis of alkylboronates from arylacetylenes and vinyl arenes
Yang, Kai,Song, Qiuling
supporting information, p. 932 - 936 (2016/02/27)
A transition-metal-free synthesis of alkylboronates, utilizing arylacetylenes or vinyl arenes and bis(pinacolato)diboron through tandem borylation and protodeboronation, has been developed. This reaction is efficient, practical and environmentally benign, leading to anti-Markovnikov products with excellent regioselectivity, broad functional group tolerance and excellent yields in both small and gram scales.
NOVEL CONDENSED PYRAZOLE DERIVATIVE AND MEDICAL USES THEREOF
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Paragraph 0299-0301; 0304, (2016/10/10)
PROBLEM TO BE SOLVED: To provide a preventive or therapeutic agent for mood disorder, anxiety disorder, schizophrenia, dementia, drug dependence or the like related to subtypes of metabolism type glutamate receptor (mGlu) 2 and 3. SOLUTION: There are prov
MediaChrom: Discovering a Class of Pyrimidoindolone-Based Polarity-Sensitive Dyes
Dell'Acqua, Monica,Ronda, Luca,Piano, Riccardo,Pellegrino, Sara,Clerici, Francesca,Rossi, Elisabetta,Mozzarelli, Andrea,Gelmi, Maria Luisa,Abbiati, Giorgio
, p. 10939 - 10954 (2015/11/18)
A small library of six polarity-sensitive fluorescent dyes, nicknamed MediaChrom, was prepared. This class of dyes is characterized by a pyrimidoindolone core fitted out with a conjugated push-pull system and a carboxy linker for a conceivable coupling wi
Click reaction as a tool to combine pharmacophores: The case of Vismodegib
Christodoulou, Michael S.,Mori, Mattia,Pantano, Rebecca,Alfonsi, Romina,Infante, Paola,Botta, Maurizio,Damia, Giovanna,Ricci, Francesca,Sotiropoulou, Panagiota A.,Liekens, Sandra,Botta, Bruno,Passarella, Daniele
, p. 938 - 943 (2015/06/08)
Abstract The design and the preparation of a small library of 1,4-diphenyl-1,2,3-triazole derivatives is reported, with the aim to obtain a new class of Hedgehog pathway inhibitors. The smoothened protein is part of the hedgehog signaling pathway that is
NAPHTHYLACETIC ACIDS
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Page/Page column 107, (2010/06/15)
The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts and esters thereof, wherein X, Q, and R1-R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
Design, synthesis, and structure-activity relationship studies of 3,4,6-triphenylpyran-2-ones as selective cyclooxygenase-2 inhibitors
Rao, P.N. Praveen,Uddin, Md. Jashim,Knaus, Edward E.
, p. 3972 - 3990 (2007/10/03)
A group of regioisomeric 3,4,6-triphenylpyran-2-ones with a MeSO 2 pharmacophore at the paraposition of either a C-3 phenyl or a C-4 phenyl substituent on the central six-membered pyran-2-one ring were prepared and evaluated in vitro for their
