88511-27-7Relevant articles and documents
Process Optimization for the Large-Scale Preparation of (2 S,3 aR,7 aS)- tert-Butyl Hexahydro-2,5-methanopyrrolo[3,2- c]pyridine-1(4 H)-carboxylate, an Intermediate for Nicotinic Acetylcholine Receptor Agonists
Jarugu, Lokesh Babu,Reddy, China Anki,Chikkananjunda, Nanjundaswamy Kanikahalli,Krishnamoorthy, Suresh,Sarvanakumar, Pon,Sankar, Ulaganathan,Arunachalam, Pirama Nayagam,McDonald, Ivar M.,Olson, Richard E.,Rampulla, Richard,Mathur, Arvind,Gupta, Anuradha
supporting information, p. 1276 - 1281 (2018/09/25)
An optimized large-scale synthesis of (2S,3aR,7aS)-tert-butyl hexahydro-2,5-methanopyrrolo[3,2-c]pyridine-1(4H)-carboxylate (1A), an important intermediate for nicotinic acetylcholine receptor agonists, is described. The key feature of the synthesis involves three transformations in a one-pot process, including debenzylation and ring hydrogenation of two fused bicyclic rings. Multihundred gram quantities of 1A were prepared.
A threonine turnstile defines a dynamic amphiphilic binding motif in the AAA ATPase p97 allosteric binding site
Burnett, James C.,Lim, Chaemin,Peyser, Brian D.,Samankumara, Lalith P.,Kovaliov, Marina,Colombo, Raffaele,Bulfer, Stacie L.,LaPorte, Matthew G.,Hermone, Ann R.,McGrath, Connor F.,Arkin, Michelle R.,Gussio, Rick,Huryn, Donna M.,Wipf, Peter
supporting information, p. 4096 - 4114 (2017/07/10)
The turnstile motion of two neighboring threonines sets up a dynamic side chain interplay that can accommodate both polar and apolar ligands in a small molecule allosteric protein binding site. A computational model based on SAR data and both X-ray and cr
AMIDO-BENZYL SULFONE AND SULFOXIDE DERIVATIVES
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Page/Page column 133; 134, (2013/09/12)
The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
PYRIDINYL AND PYRIMIDINYL SULFOXIDE AND SULFONE DERIVATIVES
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Page/Page column 85, (2013/09/12)
Disclosed are certain pyridinyl and pyrimidinyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds and methods of treatment using such compounds.
AMIDO SPIROCYCLIC AMIDE AND SULFONAMIDE DERIVATIVES
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Page/Page column 146; 147, (2013/09/12)
Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
AMIDO-BENZYL SULFONE AND SULFONAMIDE DERIVATIVES
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Page/Page column 63, (2013/09/12)
Disclosed are certain amido-benzyl sulfone and sulfonamide compounds, pharmaceutical compositions comprising such compounds, land methods of treatment using such compounds.
AMIDO-BENZYL SULFOXIDE DERIVATIVES
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Paragraph 0183, (2013/09/12)
The present invention relates to certain amido-benzyl sulfoxide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment of an NAMPT-mediated disease or condition in a subject, selected from solid or liquid tumor, rheumat
ALKYL-AND DI-SUBSTITUTED AMIDO-BENZYL SULFONAMIDE DERIVATIVES
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Paragraph 0191, (2013/09/12)
The present invention relates to certain alkyl- and di-substituted amido-benzyl sulfonamide compounds, pharmaceutical compositions comprising such compounds, and to methods of treatment of NAMPT-mediated disorders, such as diabetes, rheumatoid arthritis,
Potassium 4-iodylbenzenesulfonate: Preparation, structure, and application as a reagent for oxidative iodination of arenes
Yusubov, Mekhman S.,Yusubova, Roza Y.,Nemykin, Victor N.,Maskaev, Andrey V.,Geraskina, Margarita R.,Kirschning, Andreas,Zhdankin, Viktor V.
, p. 5935 - 5942,8 (2020/09/02)
A new hypervalent iodine(V) compound, potassium 4-iodylbenzenesulfonate, was prepared by the oxidation of 4-iodobenzensulfonic acid with Oxone in water. This potassium salt can be further converted into 4-iodylbenzenesulfonic acid by treatment with the acidic form of Amberlyst 15 in water. A single-crystal X-ray structure of potassium 4-iodylbenzenesulfonate revealed the presence of polymeric chains in the solid state due to a combination of numerous intra- and intermolecular interactions. Potassium 4-iodylbenzenesulfonate will likely find many practical applications as a thermally stable and water-soluble hypervalent iodine-based oxidant, particularly useful as a reagent for oxidative iodination of aromatic substrates. This reagent can be effectively recovered from the reaction mixture (92 % recovery) by treatment of the aqueous layer with Oxone at 60°C for 2 h, followed by filtration of the precipitate. A new hypervalent iodine(V) compound, potassium 4-iodylbenzenesulfonate, was prepared by oxidation of 4-iodobenzenesulfonic acid with Oxone in water. This new reagent promises many practical applications as a thermally stable, water-soluble and recyclable hypervalent iodine oxidant, particularly useful for oxidative iodination of aromatic substrates.
Palladium-catalyzed synthesis of 2,3-disubstituted 5-azaindoles via heteroannulation reaction and of 2-substituted 5-azaindoles through domino sila-Sonogashira/5-endo cyclization
Livecchi, Marion,Calvet, Geraldine,Schmidt, Frederic
experimental part, p. 5006 - 5016 (2012/07/03)
A general and efficient procedure for the synthesis of 2,3-disubstituted 5-azaindoles through the palladium-catalyzed heteroannulation of 4-acetamido-3-iodopyridines and diaryl-, dialkyl-, or arylalkylalkynes is described along with a study of the reactio