488123-96-2Relevant academic research and scientific papers
(Z)-Selective enol triflation of α-alkoxyacetoaldehydes: Application to synthesis of (Z)-allylic alcohols via cross-coupling reaction and [1,2]-wittig rearrangement
Kurosawa, Fumiya,Nakano, Takeo,Soeta, Takahiro,Endo, Kohei,Ukaji, Yutaka
, p. 5696 - 5703 (2015/06/16)
The stereoselective transformation of α-alkoxyacetoaldehydes to the corresponding (Z)-vinyl triflates was achieved by treatment with phenyl triflimide and DBU. The stereochemistry was explained by the "syn-effect," which was attributed primarily to an σ → π interaction. The β-alkoxy vinyl triflates obtained were applied to the stereoselective synthesis of structurally diverse (Z)-allylic alcohols via transition metal-catalyzed cross-coupling reaction and [1,2]-Wittig rearrangement.
Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B
Collins, Ian,Caldwell, John,Fonseca, Tatiana,Donald, Alastair,Bavetsias, Vassilios,Hunter, Lisa-Jane K.,Garrett, Michelle D.,Rowlands, Martin G.,Aherne, G. Wynne,Davies, Thomas G.,Berdini, Valerio,Woodhead, Steven J.,Davis, Deborah,Seavers, Lisa C. A.,Wyatt, Paul G.,Workman, Paul,McDonald, Edward
, p. 1255 - 1273 (2007/10/03)
Structure-based drug design of novel isoquinoline-5-sulfonamide inhibitors of PKB as potential antitumour agents was investigated. Constrained pyrrolidine analogues that mimicked the bound conformation of linear prototypes were identified and investigated by co-crystal structure determinations with the related protein PKA. Detailed variation in the binding modes between inhibitors with similar overall conformations was observed. Potent PKB inhibitors from this series inhibited GSK3β phosphorylation in cellular assays, consistent with inhibition of PKB kinase activity in cells.
