Unactivated C(sp3)-H hydroxylation through palladium catalysis with H2O as the oxygen source
A novel palladium catalyzed hydroxylation of unactivated aliphatic C(sp3)-H bonds was successfully developed. Different from conventional methods, water serves as the hydroxyl group source in the reaction. This new reaction demonstrates good reactivity and broad functional group tolerance. The C-H hydroxylated products can be readily transformed into various highly valuable chemicals via known transformations. Based on experimental and theoretical studies, a mechanism involving the Pd(ii)/(iv) pathway is proposed for this hydroxylation reaction.
The mechanism of caseinolytic protease (ClpP) inhibition
Catch me if you can: The ClpP protease mediates protein homeostasis and can be efficiently inhibited by β-lactones. A combination of molecular docking, mutagenesis, activity-based protein profiling, and kinetics studies now reveals the mechanism of ClpP inhibition. A hydrophobic pocket next to the active site allows binding of long aliphatic and aromatic residues. The preferred stereoisomer binds into the oxyanion hole. Copyright
Gersch, Malte,Gut, Felix,Korotkov, Vadim S.,Lehmann, Johannes,B?ttcher, Thomas,Rusch, Marion,Hedberg, Christian,Waldmann, Herbert,Klebe, Gerhard,Sieber, Stephan A.
p. 3009 - 3014
(2013/04/23)
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