300355-14-0Relevant academic research and scientific papers
Chlorotrimethylsilane and Sodium Iodide: A Useful Combination for the Regioselective Deoxygenation of Arylalkyl-α-Diketones
Yuan, Ling-Zhi,Zhao, Guangkuan,Hamze, Abdallah,Alami, Mouad,Provot, Olivier
, p. 2682 - 2691 (2017/08/16)
An efficient regioselective deoxygenation of arylalkyl-1,2-diketones by the couple trimethylsilylchloride/sodium iodide has been reported. In all cases, the deoxygenation takes place on the carbonyl group (Cα=O) proximal to the aromatic ring in methylene chloride at room temperature in good yields, furnishing a series of variously functionalized alkylbenzylketones. A large range of functional groups were well tolerated on the ortho-, meta- and para-positions by this mild process regardless of their electronic effects, demonstrating the general character of the present methodology. The trimethylsilylchloride/sodium iodide reducing process was also successfully applied to reduce α-ketoacid and α-ketoester substrates. (Figure presented.).
Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients
Sarabu, Ramakanth,Bizzarro, Fred T.,Corbett, Wendy L.,Dvorozniak, Mark T.,Geng, Wanping,Grippo, Joseph F.,Haynes, Nancy-Ellen,Hutchings, Stanley,Garofalo, Lisa,Guertin, Kevin R.,Hilliard, Darryl W.,Kabat, Marek,Kester, Robert F.,Ka, Wang,Liang, Zhenmin,Mahaney, Paige E.,Marcus, Linda,Matschinsky, Franz M.,Moore, David,Racha, Jagdish,Radinov, Roumen,Ren, Yi,Qi, Lida,Pignatello, Michael,Spence, Cheryl L.,Steele, Thomas,Tengi, John,Grimsby, Joseph
supporting information, p. 7021 - 7036 (2012/11/07)
Glucokinase (GK) activation as a potential strategy to treat type 2 diabetes (T2D) is well recognized. Compound 1, a glucokinase activator (GKA) lead that we have previously disclosed, caused reversible hepatic lipidosis in repeat-dose toxicology studies.
NITROGEN-CONTAINING FIVE-MEMBERED HETEROCYCLIC COMPOUND
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Page/Page column 105-106, (2010/03/02)
The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof. The compound of the present invention has a glucokinase activity, and is useful as a medicament such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.
CRYSTALLINE ISOPROPANOL SOLVATE OF GLUCOKINASE ACTIVATOR
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Page/Page column 9; 15, (2010/11/28)
Provided is a crystalline IPA solvate of 2(R)-(3-chloro-4-methanesulfonyl-phenyl)- 3-((R)-3-oxo-cyclopentyl)-N-pyrazin-2-yl-propionamide as a glucokinase activator which increases insulin secretion in the treatment of, for example, type II diabetes.
Heteroaromatic glucokinase activators
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, (2008/06/13)
2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
