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Synthesis, Suzuki Couplings, and Small-molecule Inhibitors
Patrick Gray
Jan 01, 0001
The goal of this research project was to design and synthesize small-molecule inhibitors using reductive amination, Suzuki coupling, and the addition of protecting groups.
small molecules INHIBITORS reductive amination Suzuki coupling Organic chemistry Physical Sciences and Mathematics
Published by: Ursinus College
Copper(i)-catalyzed sulfonylative Suzuki-Miyaura cross-coupling.
Using a simple copper(i) catalyst has allowed a high yielding sulfonylative-Suzuki-Miyaura cross-coupling reaction to be developed. The process provides a single step route to diaryl sulfones from the direct combination of aryl...
Synthesis of a novel polycyclic ring scaffold with antimitotic properties via a selective domino Heck-Suzuki reaction.
Esther Alza, Luca Laraia, Brett M Ibbeson, Súil Collins, Warren RJD Galloway, Jamie E Stokes, Ashok R Venkitaraman, David R Spring
Jan 23, 2018
The synthesis of a previously undescribed sp3-rich 6-5-5-6 tetracyclic ring scaffold using a palladium catalysed domino Heck-Suzuki reaction is reported. This reaction is high-yielding, selective for the domino process over the...
Post-synthetic modification of zinc metal-organic frameworks through palladium-catalysed carbon-carbon bond formation
Andrew D. Burrows, Laura C. Fisher, Timothy J. Mays, Sean P. Rigby, Sharon E. Ashbrook, Daniel M. Dawson
Sep 01, 2015
Post-synthetic Suzuki coupling reactions have been undertaken on the halide-functionalised metal-organic frameworks (MOFs) [Zn4O(bdc-Br)3] (bdc-Br = 2-bromo-1,4-benzenedicarboxylate, IRMOF-2) and...
Robust and reusable supported palladium catalysts for cross-coupling reactions in flow
Two novel polymer encapsulated silica supported palladium catalysts have been prepared and shown to be highly active, robust and recyclable catalysts for Heck and Suzuki–Miyaura cross coupling reactions under continuous flow...
Direct core functionalisation of naphthalenediimides by iridium catalysed C–H borylation
Catherine L. Lyall, Camilla C. Shotton, Monserrat Pérez-salvia, Dan Pantos, Simon E. Lewis
Nov 18, 2014
We report the first boron-substituted naphthalenediimides (NDIs), prepared by iridium catalysed C–H activation. When the NDI substrates bear N-benzyl substituents, the naphthyl NDI core is borylated in preference, suggestive of...
Robust and reusable supported palladium catalysts for cross-coupling reactions in flow
Two novel polymer encapsulated silica supported palladium catalysts have been prepared and shown to be highly active, robust and recyclable catalysts for Heck and Suzuki–Miyaura cross coupling reactions under continuous flow...
Post-synthetic modification of zinc metal-organic frameworks through palladium-catalysed carbon-carbon bond formation
Andrew D. Burrows, Laura C. Fisher, Timothy J. Mays, Sean P. Rigby, Sharon E. Ashbrook, Daniel M. Dawson
Sep 01, 2015
Post-synthetic Suzuki coupling reactions have been undertaken on the halide-functionalised metal-organic frameworks (MOFs) [Zn4O(bdc-Br)3] (bdc-Br = 2-bromo-1,4-benzenedicarboxylate, IRMOF-2) and...
Direct core functionalisation of naphthalenediimides by iridium catalysed C–H borylation
Catherine L. Lyall, Camilla C. Shotton, Monserrat Pérez-salvia, Dan Pantos, Simon E. Lewis
Nov 18, 2014
We report the first boron-substituted naphthalenediimides (NDIs), prepared by iridium catalysed C–H activation. When the NDI substrates bear N-benzyl substituents, the naphthyl NDI core is borylated in preference, suggestive of...
Asymmetric parental genome engineering by Cas9 during mouse meiotic exit
Mammalian genomes can be edited by injecting pronuclear embryos with Cas9 cRNA and guide RNA (gRNA) but it is unknown whether editing can also occur during the onset of embryonic development, prior to pronuclear embryogenesis....
Benzoyl side-chains push the open-circuit voltage of PCDTBT/PCBM solar cells beyond 1 V
F Lombeck, S Müllers, H Komber, SM Menke, AJ Pearson, PJ Conaghan, CR McNeill, RH Friend, M Sommer
Sep 07, 2017
The synthesis, characterization and solar cell performance of PCDTBT and its highly soluble analogue hexyl-PCDTBT with cross-conjugated benzoyl moieties at the carbazole comonomer are presented. Through the use of both model...
Asymmetric parental genome engineering by Cas9 during mouse meiotic exit
Mammalian genomes can be edited by injecting pronuclear embryos with Cas9 cRNA and guide RNA (gRNA) but it is unknown whether editing can also occur during the onset of embryonic development, prior to pronuclear embryogenesis....
Economic Value of Cultural Ecosystem Services from Recreation in Popa Mountain National Park, Myanmar
Protected areas offer diverse ecosystem services, including cultural services related to recreation, which contribute manifold to human wellbeing and the economy. However, multiple pressures from other human activities...
The Expression of TALEN before Fertilization Provides a Rapid Knock-Out Phenotype in Xenopus laevis Founder Embryos.
Kei Miyamoto, Ken-Ichi T Suzuki, Miyuki Suzuki, Yuto Sakane, Tetsushi Sakuma, Sarah Herberg, Angela Simeone, David Simpson, Jerome Jullien, Takashi Yamamoto, JB Gurdon
Nov 04, 2015
Animals Base Sequence Deoxyribonucleases Embryo Nonmammalian Eye Proteins Female Fertilization Founder Effect Gene Expression Regulation Developmental Gene Knockout Techniques Genes Lethal Homeodomain Proteins Male Microinjections Molecular Sequence Data Monophenol Monooxygenase Oocytes PAX6 Transcription Factor Paired Box Transcription Factors Phenotype RNA Messenger Repressor Proteins Sequence Alignment Sperm Injections Intracytoplasmic Transcriptional Activation Xenopus laevis
Advancing tephrochronology as a global dating tool
Layers of far-travelled volcanic ash (tephra) from explosive volcanic eruptions provide stratigraphic and numerical dating horizons in sedimentary and volcanic sequences. Such tephra layers may be dispersed over tens to...
Systematic Variation of Ligand and Cation Parameters Enables Site-Selective C-C and C-N Cross-Coupling of Multiply Chlorinated Arenes through Substrate-Ligand Electrostatic Interactions.
Use of attractive noncovalent interactions between ligand and substrate is an emerging strategy for controlling positional selectivity. A key question relates to whether fine control on molecules with multiple, closely spaced...
Examining Voluntary Engagement Barriers in Knowledge Sharing Practices for Supply Chain Innovation
Voluntary engagement (VE) creates a sense of coordination and harmonization to share knowledge. The eminence of knowledge sharing (KS) for supply chain (SC) innovation is undeniable to initiate development in products, services...
Published by: IGI Global Scientific Publishing
Mice produced by mitotic reprogramming of sperm injected into haploid parthenogenotes
Toru Suzuki, Maki Asami, Martin Hoffmann, Xin Lu, Miodrag Gužvić, Christoph A. Klein, Anthony C. F. Perry
Sep 13, 2016
Sperm are highly differentiated and the activities that reprogram them for embryonic development during fertilization have historically been considered unique to the oocyte. We here challenge this view and demonstrate that mouse...
Mice produced by mitotic reprogramming of sperm injected into haploid parthenogenotes
Toru Suzuki, Maki Asami, Martin Hoffmann, Xin Lu, Miodrag Gužvić, Christoph A. Klein, Anthony C. F. Perry
Sep 13, 2016
Sperm are highly differentiated and the activities that reprogram them for embryonic development during fertilization have historically been considered unique to the oocyte. We here challenge this view and demonstrate that mouse...
Toward the total synthesis of patellazole B
Andrew W Phillips, Matthew J Anketell, Tudor Balan, Nelson YS Lam, Simon Williams, Ian Paterson
Nov 15, 2018
The patellazoles are a family of complex marine macrolides that exhibit potent cytotoxicity against cancer cell lines. However, despite extensive characterisation efforts, their full stereochemical assignment has remained...
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