71221-49-3Relevant academic research and scientific papers
A mild and chemoselective CALB biocatalysed synthesis of sulfoxides exploiting the dual role of AcOEt as solvent and reagent
Anselmi, Silvia,Liu, Siyu,Kim, Seong-Heun,Barry, Sarah M.,Moody, Thomas S.,Castagnolo, Daniele
supporting information, p. 156 - 161 (2021/01/14)
A mild, chemoselective and sustainable biocatalysed synthesis of sulfoxides has been developed exploiting CALB and using AcOEt with a dual role of more environmentally friendly reaction solvent and enzyme substrate. A series of sulfoxides, including the drug omeprazole, have been synthesised in high yields and with excellent E-factors.
The design and synthesis of novel, phosphonate-containing transient receptor potential melastatin 8 (TRPM8) antagonists
Matthews, Jay M.,Qin, Ning,Colburn, Raymond W.,Dax, Scott L.,Hawkins, Mike,McNally, James J.,Reany, Laura,Youngman, Mark A.,Baker, Judith,Hutchinson, Tasha,Liu, Yi,Lubin, Mary Lou,Neeper, Michael,Brandt, Michael R.,Stone, Dennis J.,Flores, Christopher M.
supporting information; experimental part, p. 2922 - 2926 (2012/06/04)
A series of benzothiophene-based phosphonates was synthesized and many analogs within the series were shown to be potent antagonists of the TRPM8 channel. The compounds were obtained as a racemic mixture in 5 synthetic steps, and were tested for TRPM8 antagonist activity in a recombinant, canine TRPM8-expressing cell line using a fluorometric imaging plate reader (FLIPR) assay. Structure-activity relationships were developed initially by modification of the core structure and subsequently by variation of the aromatic substituents and the phosphonate ester. Compound 9l was administered intraperitoneally to rats and demonstrated engagement of the TRPM8 target in both prevention and reversal-modes in an icilin-induced 'wet-dog' shake model.
COLD MENTHOL RECEPTOR-1 ANTAGONISTS
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Page/Page column 55, (2012/03/12)
The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
COLD MENTHOL RECEPTOR-1 ANTAGONISTS
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Page/Page column 55, (2012/07/28)
The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
Diphenyl diselenide-assisted α-phenylthiolation of carbonyl compounds with diphenyl disulfide
Anbou, Hiroaki,Umeda, Rui,Nishiyama, Yutaka
experimental part, p. 1248 - 1250 (2012/01/31)
For the cesium carbonate-catalyzed α-phenylthiolation of carbonyl compounds with diphenyl disulfide, the yields of the α-phenylthio carbonyl compounds were dramatically improved by the addition of a catalytic amount of diphenyl diselenide.
COLD MENTHOL RECEPTOR-1 ANTAGONISTS
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Page/Page column 173-174, (2008/06/13)
The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
Homologation of aldehydes using (phenylthiomethylene) triphenylarsorane: Selective preparation of α-thiophenoxyepoxides and phenylthioenol ethers
Boubia,Mioskowski,Manna,Falck
, p. 6023 - 6026 (2007/10/02)
The title arsonium ylide reacts with aldehydes to give exclusively α-thiophenoxyepoxides in THF and phenylthioenol ethers in THF/HMPA. The former adducts are readily transformed to α-thiophenoxy carbonyls and the latter to one-carbon homologated aldehydes.
Replacement of the Activated Nitro Group by a Phenylthio Group
Miyake, Hideyoshi,Yamamura, Kimiaki
, p. 89 - 92 (2007/10/02)
The nitro group, activated by a carbonyl group, alkoxycarbonyl group or a phenyl group, can be replaced by a phenylthio group in the reaction with benzenethiol or its potassium salt.This reaction proceeds in the electron transfer mechanism, and is applicable to the general syntheses of α-phenylthio ketones, α-phenylthio carboxylic esters and α-phenylthio alkylbenzenes from primary nitro compounds.
