161014-15-9Relevant academic research and scientific papers
Thiofunctionalization of Electron-Rich Heteroarenes through Magnesiation and Trapping with Octasulfur
Vera, Gonzalo,Mangeant, Reynald,Stiebing, Silvia,Berhault, Yohann,Fabis, Frédéric,Cailly, Thomas,Collot, Valérie
, p. 5099 - 5105 (2021/09/25)
Herein we report a site-selective and thiol-free thiofunctionalization of electron-rich heteroarenes. After a selective ortho-magnesiation, the use of S8 followed by an electrophile allows direct access to S-alkyl or -aryl derivatives. In situ oxidation provides the corresponding sulfoxide and sulfone derivatives. Applying this protocol, Cerlapirdine was prepared in 4 steps with 28% overall yield. (Figure presented.).
SMALL MOLECULE CD38 INHIBITORS AND METHODS OF USING SAME
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, (2013/03/26)
The invention provides methods and compositions for inhibiting CD 38 activity, and methods of treating or preventing various disorders associated with CD38 activity.
FRICTIONLESS MOLECULAR ROTARY MOTORS
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Page/Page column 30, (2010/02/17)
A rotaxane consisting of a cucurbituril and an uncharged guest molecule, having low or null affinity therebetween is provided as well as processes for providing the same. Various uses as energy converters (“frictionless” molecular motors), biochips and biosensors using the same are also provided.
A new boronic-acid based strategy to synthesize 4(5)-(het)aryl-1H-imidazoles
Primas, Nicolas,Mahatsekake, Clément,Bouillon, Alexandre,Lancelot, Jean-Charles,Oliveira Santos, Jana Sopkovà-de,Lohier, Jean-Fran?ois,Rault, Sylvain
, p. 4596 - 4601 (2008/09/20)
This paper describes the synthesis of a new N-THP protected 5-(1H)-imidazolyl boronic acid pinacol ester and its use in Suzuki cross-coupling reactions with a wide range of (het)aryl halides to provide 4(5)-(het)aryl-1H-imidazoles.
A New Direct Glycosylation of Pyrimidine, Pyrazole, Imidazole and Purine Heterocycles via their N-tetrahydropyranyl (THP) Derivatives
Manfredini, Stefano,Baraldi, Pier Giovanni,Bazzanini, Rita,Guarneri, Mario,Simoni, Daniele
, p. 583 - 584 (2007/10/02)
Pyrimidine, pyrazole, imidazole and purine N-tetrahydropyranyl (THP) derivatives have been converted in one-pot and in a regio- and stereo-selective manner into the corresponding β-D-2',3',5'-tri-O-benzoyl ribofuranosyl nucleoside derivatives on treatment with 1-β-acetyl-2',3',5'-tri-O-benzoyl-ribofuranose, hexamethyldisilazane (HMDS), trimethylsilyl chloride (TMSCl), and trimethylsilyl triflate (TMST).
