165544-26-3Relevant academic research and scientific papers
SELECTIVE KINASE INHIBITORS
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Paragraph 0569; 0570, (2013/06/06)
Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
Conversion of α-keto esters into β,β-difluoro-α-keto esters and corresponding acids: A simple route to a novel class of serine protease inhibitors
Parisi,Gattuso,Notti,Raymo,Abeles
, p. 5174 - 5179 (2007/10/02)
The preparation of a series of β,β-difluoro-α-keto esters and corresponding acids RCF2COCO2R' (R=Me, Et, i-Pr, Bn, and Ph; R'=Et and H), designed as potential inhibitors of serine proteases, is described. The standard procedure developed consists in the initial formation of an α,α- difluoro ester from an α-keto ester, followed by a simple four-step sequence involving the synthesis of hemiacetal, cyanohydrin, and α-hydroxy ester difluorinated intermediates. This method provides an easy route to β,β- difluoro-α-keto esters and corresponding acids, via 'formal' insertion of a difluoromethylene group between the R substituent and the α-carbonyl group of a generic α-keto ester.
