A5048964740- Catalytic C–H Functionalization Methods
- Oxidative Organic Chemistry Reactions
- Synthesis and Catalytic Reactions
- Click Chemistry and Applications
- Chemical Synthesis and Analysis
- Peptidase Inhibition and Analysis
- Asymmetric Hydrogenation and Catalysis
- Synthetic Organic Chemistry Methods
- Synthesis and pharmacology of benzodiazepine derivatives
- Nanoplatforms for cancer theranostics
- Supramolecular Self-Assembly in Materials
- Luminescence and Fluorescent Materials
- Advanced Synthetic Organic Chemistry
- Alzheimer's disease research and treatments
- Radical Photochemical Reactions
- Organoboron and organosilicon chemistry
- Blood properties and coagulation
- Protein Structure and Dynamics
- Cyclopropane Reaction Mechanisms
- Advanced Nanomaterials in Catalysis
- Biotin and Related Studies
- Chemical synthesis and alkaloids
Merck & Co., Inc., Rahway, NJ, USA (United States)
2024
Princeton University
2022
The University of Tokyo
2014-2018
Japan Science and Technology Agency
2015-2018
Bunkyo University
2014-2016
Kansai University
2015
Shenyang Pharmaceutical University
2011
Abstract The first copper‐catalyzed intramolecular C(sp 3 )H and 2 oxidative amidation has been developed. Using a Cu(OAc) catalyst an Ag CO oxidant in dichloroethane solvent, proceeded at terminal methyl group, as well the internal benzylic position of alkyl chain. This reaction broad substrate scope, various β‐lactams were obtained excellent yield, even on gram scale. Use CuCl under O atmosphere dimethyl sulfoxide, however, leads to 2‐indolinone selectively by amidation. Kinetic isotope...
State-of-the-art methods in photoproximity labeling center on the targeted generation and capture of short-lived reactive intermediates to provide a snapshot local protein environments. Diazirines are current gold standard for high-resolution proximity labeling, generating aryl(trifluoromethyl) carbenes. Here, we present method access carbenes from stable diazo source via tissue-penetrable, deep red near-infrared light (600–800 nm). The operative mechanism this activation involves Dexter...
Abstract The first copper‐catalyzed intramolecular C(sp 3 )H and 2 oxidative amidation has been developed. Using a Cu(OAc) catalyst an Ag CO oxidant in dichloroethane solvent, proceeded at terminal methyl group, as well the internal benzylic position of alkyl chain. This reaction broad substrate scope, various β‐lactams were obtained excellent yield, even on gram scale. Use CuCl under O atmosphere dimethyl sulfoxide, however, leads to 2‐indolinone selectively by amidation. Kinetic isotope...
Aerobic, site-selective C(sp<sup>3</sup>)–H oxygenation using a novel <italic>N</italic>-oxyl radical directing activator (chemically reactive group) is described.
Recent studies have identified serotonylation of glutamine-5 on histone H3 (H3Q5ser) as a novel posttranslational modification (PTM) associated with active transcription. While H3Q5ser is known to be installed by tissue transglutaminase 2 (TGM2), the substrate characteristics affecting deposition mark, at level both chromatin and individual nucleosomes, remain poorly understood. Here, we show that excluded from constitutive heterochromatic regions in mammalian cells. Biochemical reveal...
Chemo- and site-selective hydrosilylation of α- or β-hydroxy amides using organocatalyst B(C6F5)3 commercially available hydrosilanes is described. This transformation operative under mild conditions tolerates a wide range functional groups. The reaction was applied for selective reduction specific amide group the therapeutically important cyclic peptide cyclosporin A, demonstrating potential usefulness this catalytic method in late-stage structural transformations drug lead molecules.
In the presence of NO<sub>x</sub> species, a regio- and oxidation state-selective aerobic methylene C(sp<sup>3</sup>)–H was realized through directing activator (DA) strategy.
The site-selective cleavage of peptide bonds is an important chemical modification that useful not only for the structural determination peptides, but also as artificial modulator peptide/protein function and properties. Here we report hydrolysis at Ser Thr positions with a high conversion yield. This relies on Sc(iii)-promoted N,O-acyl rearrangement subsequent hydrolysis. method applicable to broad scope polypeptides various functional groups, including post-translationally modified...
A stable Aβ oligomer mimic that is transformed into fibrils by a chemical stimulus, <italic>i.e.</italic>, an oxime exchange reaction, disclosed.