Search results for "Suzuki-Miyaura cross-coupling"
showing 2 items of 2 documents
3D Printed Palladium Catalyst for Suzuki-Miyaura Cross-coupling Reactions
2020
Selective laser sintering (SLS) 3d printing was utilized to manufacture a solid catalyst for Suzuki-Miyaura cross-coupling reactions from polypropylene as a base material and palladium nanoparticles on silica (SilicaCat Pd(0)R815-100 by SiliCycle) as the catalytically active additive. The 3d printed catalyst showed similar activity to that of the pristine powdery commercial catalyst, but with improved practical recoverability and reduced leaching of palladium into solution. Recycling of the printed catalyst led to increase of the induction period of the reactions, attributed to the pseudo-homogeneous catalysis. The reaction is initiated by oxidative addition of aryl iodide to palladium nano…
Identification of 2-(thiophen-2-yl)acetic Acid-Based Lead Compound for mPGES-1 Inhibition.
2021
We report the implementation of our in silico/synthesis pipeline by targeting the glutathione-dependent enzyme mPGES-1, a valuable macromolecular target in both cancer therapy and inflammation therapy. Specifically, by using a virtual fragment screening approach of aromatic bromides, straightforwardly modifiable by the Suzuki-Miyaura reaction, we identified 3-phenylpropanoic acid and 2-(thiophen-2-yl)acetic acid to be suitable chemical platforms to develop tighter mPGES-1 inhibitors. Among these, compounds 1c and 2c showed selective inhibitory activity against mPGES-1 in the low micromolar range in accordance with molecular modeling calculations. Moreover, 1c and 2c exhibited interesting IC…