A5087244012- Chemical Synthesis and Analysis
- Click Chemistry and Applications
- Sulfur-Based Synthesis Techniques
- X-ray Diffraction in Crystallography
- Synthetic Organic Chemistry Methods
- Radical Photochemical Reactions
- Microbial Natural Products and Biosynthesis
- Peptidase Inhibition and Analysis
- Crystallization and Solubility Studies
- Catalytic Cross-Coupling Reactions
- Chemical Reactions and Isotopes
- Medical Imaging Techniques and Applications
- Advanced biosensing and bioanalysis techniques
- Synthesis and Biological Activity
- Radiopharmaceutical Chemistry and Applications
- Pharmacological Effects of Natural Compounds
- Chemical Synthesis and Characterization
- RNA and protein synthesis mechanisms
- Health and Medical Research Impacts
- Diversity and Career in Medicine
- DNA and Nucleic Acid Chemistry
- Doctoral Education Challenges and Solutions
- Carbohydrate Chemistry and Synthesis
- Monoclonal and Polyclonal Antibodies Research
- Synthesis and Catalytic Reactions
Texas A&M University
2021-2022
Scripps (United States)
2020
Scripps Institution of Oceanography
2020
Torrey Pines Institute For Molecular Studies
2020
Scripps Research Institute
2017-2019
Bristol-Myers Squibb (United States)
2018
University of California, Berkeley
2017
New Mexico State University
2014-2015
C–N cross-coupling is one of the most valuable and widespread transformations in organic synthesis. Largely dominated by Pd- Cu-based catalytic systems, it has proven to be a staple transformation for those both academia industry. The current study presents development mechanistic understanding an electrochemically driven, Ni-catalyzed method achieving this reaction high strategic importance. Through series electrochemical, computational, kinetic, empirical experiments, key features have...
Phosphorothioate nucleotides have emerged as powerful pharmacological substitutes of their native phosphodiester analogs with important translational applications in antisense oligonucleotide (ASO) therapeutics and cyclic dinucleotide (CDN) synthesis. Stereocontrolled installation this chiral motif has long been hampered by the systemic use phosphorus(III) [P(III)]-based reagent systems sole practical means assembly. A fundamentally different approach is described herein: invention a...
A thermodynamic approach to peptide macrocyclization inspired by the cyclization of non-ribosomal aldehydes is presented. The method provides access structurally diverse macrocycles exploiting reactivity transient macrocyclic imines toward inter- and intramolecular nucleophiles. Reactions are performed in aqueous media, absence side chain protecting groups, tolerant all proteinogenic functional groups. Macrocyclic products bearing non-native rigidifying structural motifs, isotopic labels, a...
This Communication reports the first general method for rapid, chemoselective, and modular functionalization of serine residues in native polypeptides, which uses a reagent platform based on P(V) oxidation state. redox-economical approach can be used to append nearly any kind cargo onto serine, generating stable, benign, hydrophilic phosphorothioate linkage. The tolerates all other known nucleophilic functional groups naturally occurring proteinogenic amino acids. A variety applications...
A two-step degradation–reconstruction approach to the carbon-14 radiolabeling of alkyl carboxylic acids is presented. Simple activation via redox-active ester formation was followed by nickel-mediated decarboxylative carboxylation afford a range complex compounds with ample isotopic incorporations for drug metabolism and pharmacokinetic studies. The practicality operational simplicity protocol were demonstrated its use in an industrial setting.
Tetrachloro-N-hydroxyphthalimide tetramethyluronium hexafluorophosphate (CITU) is disclosed as a convenient and economical reagent for both acylation decarboxylative cross-coupling chemistries. Within the former set of reactions, CITU displays reactivity similar to that common coupling reagents, but with increased safety reduced cost. latter, yields, more rapid conversion, simplified procedure are possible across range reported transformations.
Complex biases may inherently limit efforts to identify predictors of success in PhD programs. Nonetheless, undergraduate performance and experience captured by the student’s GPA hold predictive value about completing a PhD. However, once past that threshold, other factors be major determinants productivity during
C–N cross-coupling is one of the most valuable and widespread transformations in organic synthesis. Largely dominated by Pd- Cu-based catalytic systems, it has proven to be a staple transformation for those both academia industry. The current study presents development mechanistic understanding an electrochemically driven, Ni-catalyzed method achieving this reaction high strategic importance. Through series electrochemical, computational, kinetic, empirical experiments key features have been...
A two-step degradation-reconstruction approach to the carbon-14 radiolabeling of alkyl carboxylic acids is presented. Simple activation via redox-active ester formation was followed by nickel-mediated decarboxylative carboxylation afford a range complex compounds with ample isotopic incorporations for drug metabolism and pharmacokinetic studies. The practicality operational simplicity protocol demonstrated its use in an industrial setting.
The first asymmetric total synthesis and revision of the relative configuration 12-membered taumycin A macrocycle is described. Key to success this work was a novel α-keto ketene macrocyclization that provided an efficient means by which access two diastereomers desired macrolide without need employ additional coupling agents or unnecessary oxidation state adjustments.
A synthetic strategy to access the fused 6-7-6 tricyclic core of hetisine-type C
<div> <p>C–N cross-coupling is one of the most valuable and widespread transformations in organic synthesis. Largely dominated by Pd- Cu-based catalytic systems, it has proven to be a staple transformation for those both academia industry. The current study presents development mechanistic understanding an electrochemically driven, Ni-catalyzed method achieving this reaction high strategic importance. Through series electrochemical, computational, kinetic, empirical experiments...
A two-step degradation-reconstruction approach to the carbon-14 radiolabeling of alkyl carboxylic acids is presented. Simple activation via redox-active ester formation was followed by nickel-mediated decarboxylative carboxylation afford a range complex compounds with ample isotopic incorporations for drug metabolism and pharmacokinetic studies. The practicality operational simplicity protocol demonstrated its use in an industrial setting.
ADVERTISEMENT RETURN TO ISSUEViewpointNEXTFunctionalized Peptides: Ideal Targets for Collaborative ChemistryJustine N. deGruyter*Justine deGruyterDepartment of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, United States*E-mail: [email protected]More by Justine deGruyterhttp://orcid.org/0000-0003-0465-8988Cite this: Biochemistry 2018, 57, 19, 2745–2746Publication Date (Web):April 27, 2018Publication History Received9 March 2018Published...
Abstract The relative stereochemistry of the taumycin macrolide is confirmed via first total synthesis aldehyde (I).
Key words cyclic dinucleotides - oligonucleotides phosphorus(V) reagents phosphorothioates